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The most potent compound, TASP0376377 (I) shows good CRTH2 antagonist potency, as well as sufficient selectivity for binding to CRTH2 over the DP1 prostanoid receptor and COX-1 and COX-2 enzymes.

Acetylated and unprotected enones derived from d -glucal reacted with trimethylsilyl cyanide in the presence of a catalytic amount of a palladium compound in 1,4-addition fashion to afford the corresponding 3-keto-glycosyl cyanides in high yield and in high α-selectivity.

Diels–Alder reaction of 2,3-bis(pinacolato)boryl-1,3-butadiene with electron-deficient alkenes and dimethyl acetylenedicarboxylate proceeded smoothly upon heating, giving rise to the corresponding ...

Treatment of (Z)-1,2,3,4-tetrakis(pinacolatoboryl)but-2-ene, prepared from 2,3-bis(pinacolatoboryl)buta-1,3-diene and bis(pinacolato)diboron, with three molar equivalents of aldehyde in toluene at 100 degrees C gave the 2,3-bis(alkylidene)alkane-1,5-anti-diol as a single stereoisomer. The reaction is applicable to both aromatic and alpha-unbranched aliphatic aldehydes. The 1,5-anti-diols were also synthesized by the one-pot preparation/triple-aldehyde addition of the tetraborylated butene. Experimental results for the stepwise treatment of the butene with two types of aldehydes suggest that the rate-determining step of the triple-aldehyde addition is the third allylation.

Cyclopropylidene lithium carbenoids reacted with bis(pinacolato)diboron in THF/Et2O at −110 °C to give various 1,1-diborylated cyclopropanes in good yields. Treatment of the diborylated cyclopropan...

(Z)-l,2,3,4-Tetraboryl-2-butene reacted with three molecules of 2,3-dialkylidene-l,5-alkanediol as a single stereoisomer. Preparation and triple addition of the butene can be effected in a single operation.

Chiral nitroxide–cyclotriphosphazene hybrid compounds such as 2,2-dinitroxide (1a), 2,2,4,4-tetranitroxide (2a), and 2,2,4,4,6,6-hexanitroxide (3a) have been prepared to examine the potentiality fo...

One of the conformational polymorphs of bis(2,6- dimethylpyridine)copper(I) perchlorate has been synthesized and its structure determined by single- crystal X-ray diffraction techniques. The crystals are monoclinic, space group Ia, with a = 14.858(3), b = 8.236(1), c = 16.308(2) A, β = 124.78(1)°, Z = 4; R was 0.070 for No= 1160 independent observed reflections. The coordination geometry around the Cu(I) atom is nearly linear with different CuN distances, CuN(1)=1.899(16) and CuN(2)= 1.953(22) A. The dihedral angle between the pyridine planes is 56.2. The relationship between the CuN- (pyridine) distance and Cu···CH3(methyl group) contacts has been discussed.

The reduction of Cu(ClO4)2·6H2O with copper wire in the presence of styrene and 2,2′-bipyridine (bipy) gave the complex [CuI(bipy)(CH2CHPh)(ClO4)] in methanol. The complex has been characterized by spectroscopic and X-ray diffraction studies. Crystals of the complex are monoclinic, space group P21/n, with a= 12.154(3), b= 14.796(4), c= 10.361(2)A, β= 111.04(2)°, and Z= 4. The geometry about the copper(I) atom is trigonal pyramidal, involving two nitrogen atoms of bipy and two carbon atoms of the olefinic moiety of styrene at equatorial positions in an approximately planar fashion and weak co-ordination to an oxygen atoms of the perchlorate anion at the axial position. The olefinic CC bond distance of the co-ordinated styrene molecule, 1.358(10)A, is slightly longer than those reported for other free olefin molecules. This slight lengthening is reflected in the 1H n.m.r. spectrum of the olefinic protons and the CC stretching frequency of the co-ordinated styrene in the Raman spectrum and suggests the importance of dπ(metal)→π*(styrene) back donation in the copper(I)–olefin bonding.