Vinxaltine sulfate, Vinfosiltine sulfate, Servier-12363, S-12363, -Drug Synthesis Database

【结构式】

【药物名称】Vinxaltine sulfate, Vinfosiltine sulfate, Servier-12363, S-12363

【化学名称】(1S)-1-[3-(O4-Deacetyl-3-demethoxycarbonylvincaleukoblastinyl)carbonylamino]-2-methylpropylphosphonic acid diethyl ester sulfate
　　　　　　[23(S)]-4-Deacetyl-3-de(methoxycarbonyl)-3-[(2-methyl-1-phosphonopropyl)carbamoyl]vincaleukoblastine diethyl ester sulfate

【CA登记号】123286-01-1, 123286-00-0 (free base)

【分子式】C₅₁H₇₄N₅O₁₄PS

【分子量】1044.22133

【开发单位】Servier (Originator)

【药理作用】Alkaloids

合成路线1

The condensation of O4-deacetyl-vinblastine carboxazide (I) with diethyl ester (+) of 1-amino-2-methylpropylphosphonic acid (II), in cold methylene chloride, gives (1S)-1-[3-(O4-deacetyl-3-demethoxycarbonylvincaleukoblastinyl) carbonylamino]-2-methylpropylphosphonic acid diethyl ester (III).

参考文献中间体

【1】 Bizzari, J.P.; Vinfosiltine Sulfate. Drugs Fut 1991, 16, 9, 822.
【2】 Lavielle, G.; Schaeffer, C.; Hautefaye, P.; Boutin, J.A.; Cudennec, C.A.; Pierré, A.; New alpha-aminophosphonic acid derivatives of vinblastine: Chemistry and antitumor activity. J Med Chem 1991, 34, 7, 1998-2003.

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)	10348	1-([(3aR,4R,5S,5aR,10bR,13aR)-3a-Ethyl-9-[(13S,15S,17S)-17-ethyl-17-hydroxy-13-(methoxycarbonyl)-1,11-diazatetracyclo[13.3.1.0(4,12).0(5,10)]nonadeca-4(12),5,7,9-tetraen-13-yl]-4,5-dihydroxy-8-methoxy-6-methyl-3a,4,5,5a,6,11,12,13a-octahydro-1H-indolizino[8,1-cd]carbazol-5-yl]carbonyl)-1,2-triazadien-2-ium		C₄₃H₅₃N₇O₇	详情	详情
(II)	14215	diethyl (1S)-1-amino-2-methylpropylphosphonate		C₈H₂₀NO₃P	详情	详情

Extended Information