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SYNTHESIS N-PROTECTED AMINO ACIDS, ESPECIALLY N-BOC-L-PROPARGYLGLYCINE BY ZINC-MEDIATED ADDITION OR ORGANIC HALIDES TO GLYCINE CATION EQUIVALENT
SYNTHESIS N-PROTECTED AMINO ACIDS, ESPECIALLY N-BOC-L-PROPARGYLGLYCINE BY ZINC-MEDIATED ADDITION OR ORGANIC HALIDES TO GLYCINE CATION EQUIVALENT
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机译:通过锌介导的加成或有机卤化物合成相当于N-BOC-L-脯氨酰甘氨酸的甘氨酸阳离子等效物
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摘要
A method is described for synthesis of N-Boc-L- propargylglycine, a key intermediate used in the preparation of high- potency, orally-active renin inhibitors. This method involves reaction of an organic halide with a glycine cation equivalent, such as methyl N-Boc- 2-acetoxyglycine, in the presence of zinc dust to give Boc-protected amino acid derivatives in high yield. Typically useful organic halides are allylic, benzylic and propargylic halides. Resolution of methyl N-Boc- propargylglycine with . alpha.-chymotrypsin provides N-Boc-L- propargylglycine in high yield.
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