Koji Koyano

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An improved synthetic method for triplet drugs with the 1,3,5-trioxazatriquinane skeleton was developed that used p-toluenesulfonylmethyl isocyanide (TosMIC) instead of 1,3-dithiane. Using the improved method, we synthesized compounds with two identical pharmacophore units and an epoxymethano group, that is, capped homotriplets. Among the synthesized capped(More)
Novel double-capped triplet drugs, which have one pharmacophore unit and two epoxymethano or dimethylepoxymethano structures (termed cap or diMe-cap structures, respectively) were synthesized. Key intermediate oxazoline 16 derived from acetone enabled the effective synthesis of double-capped triplets. SYK-134 (7a) and SYK-135 (8a) with N-cyclopropylmethyl(More)
C10H18N2O5S.H2O, Mr = 296.39, monoclinic, P2(1), a = 19.600 (1), b = 7.480 (1), c = 5.061 (1) A, beta = 94.74 (1) degree, V = 739.445 (1) A3, Z = 2, Dm = 1.31, Dx = 1.331 g cm-3, Cu K alpha, lambda = 1.54178 A, mu = 21.4 cm-1, F(000) = 316, room temperature, R = 0.057 for 1263 reflections. The molecule adopts an extended form. The molecules are arranged so(More)
The crystals of 1alpha24(R)dihydroxy-vitamin D3 monohydrate, C27O3H44.H2O are orthorhombic in the space group P2(1)2(1)2(1) with cell dimensions a=25.719, b=42.572, c=9.851A and Z=16. The asymmetric unit consists of two subunits with b/8, and each subunit contains a dimer in which two molecules are hydrogen-bonded through water molecules into(More)
A series of 5,6,6a,8,9,11a-hexahydroanaphth[1',2':4,5]imidazo[2,q-b]thiazoles (17 and 20) and 5,6,6a,9,10,11a-hexahydronaphth[2',1':4,5]imidazo[2,1-b]thiazoles has been synthesized with cis- and/or trans-1,2-diamino-1,2,3,4-tetrahydronaphthalenes as the key intermediates and subsequently evaluated for immunological activity (effects on antibody formation(More)
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