首页> 外国专利> HOLICHONDRIN B DERIVATIVES, CONDENSED PYRAN DERIVATIVES (VARIANTS), HYDROGENATED FURAN DERIVATIVES, HYDROGENATED PYRAN DERIVATIVES, GALICHONDRIN B ENONE DERIVATIVES AND NORGALICHONDRIN ENONE DERIVATIVES

HOLICHONDRIN B DERIVATIVES, CONDENSED PYRAN DERIVATIVES (VARIANTS), HYDROGENATED FURAN DERIVATIVES, HYDROGENATED PYRAN DERIVATIVES, GALICHONDRIN B ENONE DERIVATIVES AND NORGALICHONDRIN ENONE DERIVATIVES

机译:HOLICHONDRIN B衍生物,缩合吡喃衍生物(变体),加氢的呋喃衍生物,加氢的吡喃衍生物,GALICHONDRIN B烯酮衍生物和降冰片软骨素烯酮衍生物

摘要

FIELD: medicine, particularly, manufacture of antitumor drugs. SUBSTANCE: antitumor drugs have structural formula I wherein R1 and R2 are C1-6-alkyl; A is unprotected of protected group of formula: CH2CH2OH; B is unprotected or protected OH; m=n=1. Intermediate compounds have structural formula II wherein R1 is C1-6-alkyl; R2 is protected OH, R3 is CHO, CO2D wherein D is C1-5-alkyl; R4 is unprotected or protected OH; R5 is protected or unprotected OH or protected CH2CH2OH; structural formula III wherein X is OH, R1,R2,R3 are protected OH; R4 is CO2D in which D is C1-C5-alkyl; structural formula IV wherein R1-R5 is protected OH, R6 is oxygen, R7-R8 is C1-5 alkyl; X is halogen; structural formula V wherein R1-R6 is protected OH, R4 is oxygen, R5-R6 is C1-5- alkyl; R7 is CO2D in which D is C1-5-alkyl; X is halogen; structural formula VI wherein R1-R6 is protected OH; R8-R11 are C1-5-alkyl; R12-R13 are methylidene; R14-R15 is oxygen; structural formula VII wherein R1-R4 is protected OH; R5-R8 are -C1-5-alkyl; R9-R10 are methylidene; R11 is CO2D in which D is -C1-5 alkyl; R12 и R13 are oxygen atom. EFFECT: improved properties of the title compounds. 17 cl, 3 dwg, 12 ex, 2 tbl
机译:领域:医学,尤其是抗肿瘤药的制造。物质:抗肿瘤药物具有结构式I,其中R 1 和R 2 是C 1-6 -烷基; A不受保护的式为CH 2 CH 2 OH的保护基; B是未保护的或未保护的OH; m = n = 1。中间体化合物具有结构式II,其中R 1 是C 1-6 -烷基; R 2 是受保护的OH,R 3 是CHO,CO 2 D,其中D是C 1-5 -烷基; R 4 是未保护的或未保护的OH; R 5 是受保护或不受保护的OH或受保护的CH 2 CH 2 OH; X为OH,R 1 ,R 2 ,R 3 的结构式III为被保护的OH; R 4 为CO 2 D,其中D为C 1 -C 5 -烷基;结构式IV其中R 1 -R 5 是被保护的OH,R 6 是氧,R 7 -R 8 是C 1-5 烷基; X是卤素;结构式V其中R 1 -R 6 是被保护的OH,R 4 是氧,R 5 -R 6 是C 1-5 -烷基; R 7 为CO 2 D,其中D为C 1-5 -烷基; X是卤素;结构式VI其中R 1 -R 6 是被保护的OH; R 8 -R 11 是C 1-5 -烷基; R 12 -R 13 为亚甲基; R 14 -R 15 是氧;结构式其中R 1 -R 4 是被保护的OH; R 5 -R 8 是-C 1-5 -烷基; R 9 -R 10 为亚甲基; R 11 为CO 2 D,其中D为-C 1-5 烷基; R 12 和R 13 是氧原子。效果:改善了标题化合物的性质。 17厘升,3载重吨,12吨,2汤匙

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