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【结 构 式】

【分子编号】27037

【品名】(2R,6S,9S,11R,12R,14aS,15S,16S,20S,23S,25aS)-9-Amino-23-[(1S,2S)-2-[4-(dibenzylphosphoryloxy)phenyl]-1,2-dihydroxyethyl]-2,11,12,15-tetrahydroxy-6,20-bis(1(R)-hydroxyethyl)-.16-methyloctadecahydro-1H-dipyrrolo[2,1-c:2,1-l][1,4,7,10,13,16]hexaazacyclohenicosine-5,8,14,19,22,25-hexaone

【CA登记号】

【 分 子 式 】C48H64N7O18P

【 分 子 量 】1058.046302

【元素组成】C 54.49% H 6.1% N 9.27% O 27.22% P 2.93%

与该中间体有关的原料药合成路线共 1 条

合成路线1

该中间体在本合成路线中的序号:(III)

The synthesis of LY-307853 (the phosphate prodrug of LY-303366) has been performed: The phosphorylation of LY-303366 (I) with tetrabenzyl pyrophosphate (II) by means of LiOH in DMF gives dibenzyl phosphate (III), which is finally debenzylated by hydrogenation with H2 over Pd/C in the presence of sodium acetate.

1 Udodong, U.E.; et al.; Studies on the phosphorylation of LY303366. Tetrahedron Lett 1998, 39, 34, 6115.
中间体序号 中间体编号 品名 CAS号 分子式 供应商 用于合成
(I) 16118 (2R,6S,9S,11R,12R,14aS,15S,16S,20S,23S,25aS)-9-amino-23-[(1S,2S)-1,2-dihydroxy-2-(4-hydroxyphenyl)ethyl]-2,11,12,15-tetrahydroxy-6,20-bis[(1R)-1-hydroxyethyl]-16-methylhexadecahydro-1H-dipyrrolo[2,1-c:2,1-l][1,4,7,10,13,16]hexaazacyclohenicosine-5,8,14,19,22,25(9H,25aH)-hexone C34H51N7O15 详情 详情
(II) 27036 Tetrabenzyl diphosphate; Tetrabenzyl pyrophosphate; Pyrophosphoric acid tetrabenzyl ester; 1,1,3,3-tetrakis(benzyloxy)-3-oxo-1lambda(5),3lambda(5)-diphosphoxan-1-one 990-91-0 C28H28O7P2 详情 详情
(III) 27037 (2R,6S,9S,11R,12R,14aS,15S,16S,20S,23S,25aS)-9-Amino-23-[(1S,2S)-2-[4-(dibenzylphosphoryloxy)phenyl]-1,2-dihydroxyethyl]-2,11,12,15-tetrahydroxy-6,20-bis(1(R)-hydroxyethyl)-.16-methyloctadecahydro-1H-dipyrrolo[2,1-c:2,1-l][1,4,7,10,13,16]hexaazacyclohenicosine-5,8,14,19,22,25-hexaone C48H64N7O18P 详情 详情
Extended Information