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【结 构 式】

【分子编号】56833

【品名】(2S)-2-({4-[{[(6R)-2-amino-4-oxo-1,4,5,6,7,8-hexahydro-6-pteridinyl]methyl}(formyl)amino]benzoyl}amino)pentanedioic acid

【CA登记号】

【 分 子 式 】C20H23N7O7

【 分 子 量 】473.4456

【元素组成】C 50.74% H 4.9% N 20.71% O 23.66%

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:(XXIV)

In an alternative enzymatic synthesis, exposure of the diastereoisomeric (6R,S)-tetrahydrofolates (VIIa-b), with a recombinant enzymatic domain as the source of 10-formyltetrahydrofolate synthetase activity, led to the diastereoselective formylation the (6S) tetrahydrofolate at the 10-N (XXIV), while leaving unchanged the unnatural (6R) isomer (XXIII). The chiral 10-formyl tetrahydrofolate (XXIV) was subsequently isomerized to (6S)-5-formyltetrahydrofolate either under acidic conditions, via formation of the intermediate 5,10-methenyl derivative (III) (22), or in the presence of a source of cyclohydrolase activity.

1 Pelletier, J.N.; McKenzie, R.E.; Methenyltetrahydrofolate cyclohydrolase catalyzes the synthesis of (6S)-5-formyltetrahydrofolate. Bioorg Chem 1996, 24, 3, 220.
2 Schlingmann, G.; Rosenfeld, S.A. (Wyeth); Process for the preparation of optically pure diastereoisomers of tetrahydrofolate cpds.. EP 0432441 .
中间体序号 中间体编号 品名 CAS号 分子式 供应商 用于合成
(VIIa) 56817 (2S)-2-{[4-({[(6S)-2-amino-4-oxo-1,4,5,6,7,8-hexahydro-6-pteridinyl]methyl}amino)benzoyl]amino}pentanedioic acid C19H23N7O6 详情 详情
(VIIb),(XXIII) 56832 (2S)-2-{[4-({[(6R)-2-amino-4-oxo-1,4,5,6,7,8-hexahydro-6-pteridinyl]methyl}amino)benzoyl]amino}pentanedioic acid C19H23N7O6 详情 详情
(III) 56814 (6aR)-3-amino-8-[4-({[(1S)-1,3-dicarboxypropyl]amino}carbonyl)phenyl]-1-oxo-1H,4H,5H,6H,6aH,7H,8H-imidazo[1,5-f]pteridin-10-ium C20H22N7O6 详情 详情
(XXIV) 56833 (2S)-2-({4-[{[(6R)-2-amino-4-oxo-1,4,5,6,7,8-hexahydro-6-pteridinyl]methyl}(formyl)amino]benzoyl}amino)pentanedioic acid C20H23N7O7 详情 详情
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