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Synthesis of optically active dodecaborate-containing L-amino acids for BNCT.

机译:用于BNCT的含旋光性十二酸酯的L-氨基酸的合成。

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摘要

A convenient and simple synthetic method of dodecaboratethio-L-amino acid, a new class of tumor-seeking boron carrier for BNCT, was accomplished from S-cyanoethylthioundecahydro-closo-dodecaborate (S-cyanoethyl-(10)BSH, [(10)B(12)H(11)](2-)SCH(2)CH(2)CN) and bromo-L-alpha-amino acids by nearly one step S-alkylation. An improved synthesis of S-cyanoethyl-(10)BSH, a key starting compound for S-alkylation, was also performed by Michael addition of (10)BSH with acryronitrile in high yield. Four kinds of new dodecaboratethio-L-amino acids were obtained in optically pure form without the need for any optical resolution.
机译:从S-氰基乙基硫代十一碳二氢-十二烷酸酯(S-氰基乙基-(10)BSH,[(10) B(12)H(11)](2-)SCH(2)CH(2)CN)和溴-L-α-氨基酸通过近一个步骤的S-烷基化。 S-氰基乙基-(10)BSH(一种用于S-烷基化的关键起始化合物)的改进合成方法也可以通过高产率地将(10)BSH与丙烯腈进行迈克尔加成反应来进行。以光学纯的形式获得了四种新的十二硼酸硫代-L-氨基酸,而无需任何光学拆分。

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