A new, efficient, two step procedure for the preparation of the antineoplastic agent sparfosic acid
A new, efficient, two step procedure for the preparation of the antineoplastic agent sparfosic acid
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DOI：
10.1080/00397919708003363
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发表时间：
1997-01-01
影响因子：
2.1
通讯作者：
Cordi, AA
中科院分区：
文献类型：
--
作者：
Morris, AD;Cordi, AA
司巴膦酸可以容易地以两个步骤和优异的产率从市售原料L-天冬氨酸二叔丁酯盐酸盐和二乙基膦酰基乙酸的缩合，然后在温和条件下使用溴三甲基硅烷进行酸性官能团的四重脱保护来制备。
Sparfosic acid can easily be prepared in two steps and in excellent yield from condensation of the commercially available starting materials L-aspartic acid di-tert-butyl ester hydrochloride and diethylphosphonoacetic acid, followed by a quadruple deprotection of acidic functions under mild conditions using bromotrimethylsilane.