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O-Alkylhydroxylamines, particularly O-methylhydroxylamine, aminate nitroarenes in the presence of a strong base and a copper catalyst to give aminonitroarenes in good yields. ortho- or para-Amination with respect to the nitro group takes place, and in some cases the ortho-aminated product is preferentially obtained. With 3-substituted nitrobenzenes where the substituent has a lone pair of electrons, preferential amination occurs at the 2-position to give the sterically most congested 3c–f, 14 and 22g.

A 78-year-old male with sigmoid colon cancer underwent sigmoidectomy. The lesion was se, p1(+), n1, and Stage IV. Oral UFT therapy was performed, but was replaced with oral S-1 therapy 1 year and 6 months after surgery. Three months later, lung metastases 2.0 x 1.5 cm and 0.6 x 0.6 cm were found by chest CT in right S10a and S5b, respectively. Since the patient did not wish surgery, the treatment was changed to oral UFT/Leucovorin(LV)therapy(UFT 300 mg/ LV 75 mg, 4-week administration and 1-week no-administration periods). After 2 courses, chest CT showed disappearance of both lung metastases, indicating complete remission. Oral UFT/LV therapy is convenient because of the oral route. Adverse reactions are few, and the therapeutic effect has been reported to be comparable to that of intravenous 5-FU/LV therapy. Also, in this patient, no adverse reaction was noted, and complete remission was maintained until the patient died of another disease 31 months after the beginning of oral UFT/LV therapy.

Described is a 59 year old Japanese man With malignant lymphoma involving the stomach, duodenum, terminal ileum, colon and rectum, who developed early gastric carcinoma. Repeated gastroduodenoscopy revealed various appearances of the gastrointestinal involvement in malignant lymphoma, such as giant folds, polypoid lesions, and ulcerations, in addition to a depressed lesion of early gastric carcinoma. Colonoscopy also showed multiple polypoid lesions throughout the large bowel. Though the gastrointestinal involvement in malignant lymphoma is not rare, diffuse multiple polypoid lesions in the entire large bowel as seen in our case have rarely been endoscopically described. The coexistance of malignant lymphoma and gastric carcinoma in our case might be only a coincidence, though some reports of an increasing incidence of second tumors in patients with malignant lymphoma have been published. Further consideration will be needed as to the relationship between malignant lymphoma and the occurence of a second malignancy.

We evaluated the efficacy and tolerability of a dual therapy with rabeprazole and amoxicillin (AMX) as an empiric third-line rescue therapy. In patients with failure of first-line treatment with a proton pump inhibitor (PPI)-AMX-clarithromycin regimen and second-line treatment with the PPI-AMX-metronidazole regimen, a third-line eradication regimen with rabeprazole (10 mg q.i.d.) and AMX (500 mg q.i.d.) was prescribed for 2 wk. Eradication was confirmed by the results of the 13C-urea breath test (UBT) at 12 wk after the therapy. A total of 46 patients were included; however, two were lost to follow-up. The eradication rates as determined by per-protocol and intention-to-treat analyses were 65.9% and 63.0%, respectively. The pretreatment UBT results in the subjects showing eradication failure; those patients showing successful eradication comprised 32.9 ± 28.8 permil and 14.8 ± 12.8 permil, respectively. The pretreatment UBT results in the subjects with eradication failure were significantly higher than those in the patients with successful eradication (P = 0.019). A low pretreatment UBT result (≤ 28.5 permil) predicted the success of the eradication therapy with a positive predictive value of 81.3% and a sensitivity of 89.7%. Adverse effects were reported in 18.2% of the patients, mainly diarrhea and stomatitis. Dual therapy with rabeprazole and AMX appears to serve as a potential empirical third-line strategy for patients with low values on pretreatment UBT.

Homogeneous hydrogenation of 2-phenyl-3-methyl-2-butenoic acid derivatives in the presence of a catalytic amount of such chiral phosphine-rhodium complexes as Rh/(R)-BINAP, Rh/(R)-, or (S)-Cy-BINAP, Rh/(R)-p-tolyl-BINAP, and Rh/(R)-p-methoxy-phenyl-BINAP afforded the corresponding phenylacetic acid derivatives in high enantiomeric excesses and in quantitative chemical yields. The optically active phenylacetic acid derivatives are useful intermediates of agrochemicals and pharmaceuticals.

A set of experimental system for the study on the root system-soil interaction for laboratory work was presented. This system consisted of the following apparatuses and associating techniques for operation; (1) a handy-type root box covered with a mirror sheet, (2) a pinboard which enabled sampling of the root system in the root box soil as it stood in the soil, (3) a piece of holed polyethylene sheet for handling during the sampling of the root system and preserving the root system without impairment and disarrangement after sampling, (4) a transmitted light box for taking photograph of the root system. Techniques associating with those apparatuses consisted of the soil filling up into the root box, supplying water to the root box, washing out the root system from soil, and staining the sampled root system.Distribution patterns of soil porosity and moisture, and daily changes of soil temperature in the root box soil, were determined. Our soil filling-up technique gave high reproducibility as well as uniform porosity distribution in the root box soil with small difference among the root boxes. No significant differences were found in the soil moisture content at a given depth of horizontal soil layer. When the root box was put into the trench, the soil temperature in the root box was closer to that of a natural soil profile than when it was placed on the ground. Upland rice and maize were grown in the root box placed in the trench. Root systems sampled showed considerably uniform profiles among triplicated plants for both species. These results demonstrate the significance of preparation and control techniques of soil environments for the study on root system-soil interaction.

Serum pepsinogen levels were measured in 137 stomach cancer patients and compared with those of 288 normal cancer-free subjects. The serum pepsinogen levels of stomach cancer patients, especially pepsinogen I and the pepsinogen I/pepsinogen II ratio were significantly lower than those of normal controls and correlated well with the extent of chronic gastritis associated with the cancerous stomach. These results were in good accordance with the results of previous studies indicating that the cancer derived from the stomach where chronic gastritis/intestinal metaplasia is extensive. The high sensitivity and specificity of this non-invasive serum test to detect chronic gastritis suggested the possibility of its application to the mass screening of stomach cancer.

By treating of the oligoethylene glycol monocarboxymethyl ethers with p-toluenesulfonyl chloride in the presence of alkali metal carbonates, novel macrocyclic polyether-monoester compounds were obtained in moderate yield.

Described is a 49-year-old Japanese male who developed an ascending colon stenosis secondary to perforated appendicitis. The patient was examined at our hospital because of an abdominal pain and the presence of a firm mass in the right flank. A barium enema and colonoscopic examination revealed an ascending colon stenosis with multiple nodular elevations. On laparotomy, an inflammatory mass, originating from a ruptured appendix, was found adhered to the cecum and the ascending colon. Thus, a right hemicolectomy was performed. Microscopic examination revealed a periappendiceal abscess with marked submucosal fibrosis and lymphoid hyperplasia of the ascending colon and cecum. Large intestinal stenosis is a rare complication of appendicitis, and there have been only a few reported cases involving the ascending and sigmoid colon, and the rectum. In these cases, however, the polypoid lesions as seen in our case have never been described. In reviewing the literature, we found only two other cases in which a coarse or a polypoid lesion, similar to our case, was noted in the cecum, though the mucosal change was localized and luminal stenosis did not occur. Thus, when a patient with an ascending colon stenosis is encountered, a possibility of periappendiceal abscess must be kept in mind.

Monoclonal antibodies were used to examine the immunohistochemical expression of pepsinogens I and II in 31 early and 76 advanced gastric cancers. Of the 107 carcinomas studied, 19 contained pepsinogen II and only 3, found exclusively in pepsinogen II-positive cases, contained pepsinogen I. Gastric cancer produces pepsinogen II more frequently than pepsinogen I, and production of the latter is significantly associated with the former. Histologically, there were 54 intestinal-type and 53 diffuse-type cancers. The former produced pepsinogen II more frequently than the latter. In the diffuse type, the four pepsinogen II-positive cases were found exclusively in females. Although the pepsinogen expression was independent of the macroscopic features in advanced gastric cancer, it was found that the protruded-type early gastric cancer produced pepsinogen II more frequently than the depressed type. Incidences of pepsinogen positivity were not different between early and advanced gastric cancers or between cancers with or without lymph node metastasis, suggesting that production of pepsinogen is independent of tumor growth.

A new facile method of synthesizing crown ethers from oligoethylene glycols by treating them with arenesulfonyl or alkanesulfonyl chlorides in the presence of alkali metal hydroxide or alkoxide was described. 15-Crown-5 and 21-crown-7 were synthesized from pentaethylene glycol and heptaethylene glycol respectively in good yields, while 18-crown-6 was obtained from both hexaethylene glycol and triethylene glycol. Although the main product was 24-crown-8 in the reaction of tetraethylene glycol/TsCl/Na(K)OH in dioxane, 12-crown-4 was obtained in a moderate yield from the reaction of tetraethylene glycol/benzenesulfonyl chloride/t-BuOLi in t-BuOH. Furthermore, the analogous treatment of PEG 200 afforded a mixture of 15-, 18-, 21-, and 24-crown ethers. The reaction conditions were investigated, and the scope of the reaction was discussed.

3-Substituted 2-oxo crown ethers and a novel dioxo crown ether with a point symmetry were synthesized by the cyclization of the corresponding substituted oligoethylene glycol monocarboxymethyl ethers using benzenesulfonyl chloride in the presence of alkali metal carbonates. The reaction mechanism was discussed. Their stability constants toward sodium and potassium cations were determined and the relation between their structures and complexing properties was discussed.

1. Spontaneous mouse leukemia began to develop at 6 months and its maximum incidence was observed at 9 months of age.2. Of mice inoculated at less than 24 hours of age with cell-free filtrates extracted from AKR leukemic livers, spleens, and lymph nodes, 39.1% developed leukemia within 6 months. The incidence of leukemia for two groups of mice, 24 to 48 hours old and 48 to 72 hours old, was equally 25%. Very seldom leukemia resulted in mice inoculated at 6 to 48 days of age. There was a 2-month acceleration in the development of leukemia, however, in comparison with the control group.3. Whereas more females than males developed leukemia before 6 months following inoculation, after that time the reverse was the case.4. Leukemogenic activity of brain extracts was weaker than that of lymph node extracts.5. The second cell-free passage caused more leukemias than the first cell-free passage within 6 months.6. At autopsy there were two distinct types of leukemic involement, thymic and lymph node, and also transitional types of the two.7. The peripheral leukocyte count ranged in the majority of cases from 20, 000 to 30, 000per cu mm, rarely reaching 80, 000per cu mm. In differential counts, there were 1% to 52% lymphoblasts. Some leukemic mice showed an increase of cells of the neutrophilic series. Nucleated red cells were also present.8. In bone marrow, lymph node, thymus, and spleen, lymphoblasts were of the predominant cell type.9. In vitro tissue culture of lymph node, bone marrow, and spleen produced an identical growth pattern with that of acute lymphatic leukemia in human beings.10. The chromosomes studied in spontaneous AKR leukemia were 40 in number and rod-shaped, showing no aberrations from the normal counterparts.11. The first cell-free passage resulted in one of the mice in the development of myelogenous leukemia. The second cell-free passage from the myelogenous leukemia induced lymphatic leukemia in one of the mice injected.12. Lymphatic leukemia, once converted to the ascitic form, was subsequently maintained in the ascitic form by successive intraperitoneal transplantation.

ABS>The incidence of leukemia in RF mice exposed to a single whole-body irradiation of 350 r x-rays was 77.4%, in 41 out of 53 animals. In all, 20 developed the thymic and 20 the non-thymic lymphocytic leukemia, while only one developed myelogenous leukemia. The incidence of leukemia by 20- methylcholanthrene painting was 88% in 22 out of 25 animals. Of them, 12 developed lymphocytic leukemia and 10 myelogenous leukemia. Cell-free filtrates from the leukemic mice, which were induced by a single whole-body x irradiation, were inoculated to the newborn mice of the same strain less than 16 hours old. Two (18.7%) of the twelve inoculated animals developed leukemia on the 357th and 374th days, respectively, after the inoculation. Attempts to inoculate cell-free filtrate from 20-methylcholanthrene-induced leukemic RF mice to newborn mice of the same strain were successful. Cell-free filtrate from the myelogenous leukemic mouse caused lymphocytic leukemia in one of three inoculated mice. This is suggestive of the possibility of transformation of the type of leukemia during cell-free transmission. Virus-like particles were demonstrated by electron microscope in the lymph nodes of 20-methylcholanthrene-induced leukemic mice. The results suggest that x-ray and chemical carcinogens may act to induce leukemia or mammary carcinomamore » by the activation of a latent virus naturally resident in the RF mouse. (P.C.H.)« less

A new facile method of synthesizing crown ethers from oligoethylene glycols by treating them with arenesulfonyl or alkanesulfonyl chlorides in the presence of alkali metal hydroxide or alkoxide was described. 15-Crown-5 and 21-crown-7 were synthesized from pentaethylene glycol and heptaethylene glycol respectively in good yields, while 18-crown-6 was obtained from both hexaethylene glycol and triethylene glycol. Although the main product was 24-crown-8 in the reaction of tetraethylene glycol/TsCl/Na(K)OH in dioxane, 12-crown-4 was obtained in a moderate yield from the reaction of tetraethylene glycol/benzenesulfonyl chloride/t-BuOLi in t-BuOH. Furthermore, the analogous treatment of PEG 200 afforded a mixture of 15-, 18-, 21-, and 24-crown ethers. The reaction conditions were investigated, and the scope of the reaction was discussed.

3-Substituted 2-oxo crown ethers and a novel dioxo crown ether with a point symmetry were synthesized by the cyclization of the corresponding substituted oligoethylene glycol monocarboxymethyl ethers using benzenesulfonyl chloride in the presence of alkali metal carbonates. The reaction mechanism was discussed. Their stability constants toward sodium and potassium cations were determined and the relation between their structures and complexing properties was discussed.

Sulfur or nitrogen analogues of monooxo crown ethers were prepared via intramolecular cyclization of the corresponding thia or aza oligoethylene glycol carboxylmethyl ethers by using benzenesulfonyl chloride in the presence of alkali metal carbonates.