L-苯甘氨酰胺的制备

Preparation of L-Phenylglycine Amide

L-苯甘氨酰胺（1）是合成手性药物的重要中间体，可作为手性合成子用于制备血管舒缓激肽B1受体拈抗剂3-甲酰胺基-5-苯乙酰胺基吡唑类化合物。以及半胱氨酸蛋白酶Ⅰ和Ⅱ抑制剂埋。等；也可作为手性助剂用于合成含伯氨基的手性化合物，如β-氨基酸类降血糖药西他列汀（sitagliptin）。和螺环取代的苯并咪唑类质子泵抑制剂等。

L-Phenylglycine amide was prepared from L-phenylglycine via esterification in methanol to give L-phenylglycine methyl ester hydrochloride, followed by amidation in ammonia with an overall yield of about 65 %.