摘要:
A method is described for synthesis of N-protected amino acids, especially 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.
摘要:
This invention relates to compounds having formula (I) or pharmaceutically acceptable salts thereof which are useful in the inhibition of platelet aggregation, to pharmaceutical compositions containing such compounds, and to a method of inhibiting platelet aggregation in mammals by administering such compounds and compositions.