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发明公开
CN110317153A 一种Nα-芴甲氧羰基-N',N''-二甲酸丙烯基-L-精氨酸的制备方法 无效 - 撤回

一种Nα-芴甲氧羰基-N',N''-二甲酸丙烯基-L-精氨酸的制备方法
摘要：
本发明公开了一种Nα-芴甲氧羰基-N',N''-二甲酸丙烯基-L-精氨酸的制备方法，主要解决原工艺中的复杂性，周期长，成本高等技术问题。本发明采用的技术方案是：一种Nα-芴甲氧羰基-N',N''-二甲酸丙烯基-L-精氨酸的制备方法，具体包括以下步骤：第一步，将L-精氨酸和叔丁氧羰基供体的丙酮溶液混合制备成Nα-叔丁氧羰基-L-精氨酸；第二步，将Nα-叔丁氧羰基-L-精氨酸和甲酸丙烯基供体及催化剂混合于THF中，再有机碱作用下，经催化反应制得Nα-叔丁氧羰基-N',N''-二甲酸丙烯基-L-精氨酸；第三步，将Nα-叔丁氧羰基-N',N''-二甲酸丙烯基-L-精氨酸加入叔丁氧羰基的脱保护试剂脱除叔丁氧羰基后制备成N',N''-二甲酸丙烯基-L-精氨酸盐酸盐；第四步，将N',N''-二甲酸丙烯基-L-精氨酸盐酸盐和芴甲氧羰基氨基保护剂的丙酮溶液混合制备得到Nα-芴甲氧羰基-N',N''-二甲酸丙烯基-L-精氨酸。
摘要（英）：

The invention discloses an N-alpha-fluorenylmethoxycarbonyl-N',N''-diformyl allyl-L-arginine preparation method and mainly solves technical problems of complexity, long period, high cost and the likein an original process. The technical scheme includes steps: step one, mixing L-arginine with acetone solution of a t-butyloxycarboryl donor to obtain N-alpha-t-butyloxycarboryl-L-arginine; step two,mixing N-alpha-t-butyloxycarboryl-L-arginine, a formic allyl donor and a catalyst in THF, and performing catalytic reaction under the action of organic alkali to obtain N-alpha-t-butyloxycarboryl-N',N''-diformyl allyl-L-arginine; step three, adding the N-alpha-t-butyloxycarboryl-N',N''-diformyl allyl-L-arginine into a t-butyloxycarboryl deprotection reagent to remove t-butyloxycarboryl to obtain N',N''-diformyl allyl-L-arginine monohydrochloride; step four, mixing the N',N''-diformyl allyl-L-arginine monohydrochloride with acetone solution of a fluorenylmethoxycarbonyl amino protection agent to obtain N-alpha-fluorenylmethoxycarbonyl-N',N''-diformyl allyl-L-arginine.

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