Hänsicke A, Krause E, Bienert M, Schmidt M, Kobert S, Schellenberger V, Jakubke H D, Kaufmann K D
Berlin-Chemie AG, Berlin.
Biomed Biochim Acta. 1991;50(10-11):S201-4.
D-Xaa6-GnRH analogs (Xaa: Ala, Nal1), Phe, Ser(tBu), Trp) were prepared by chymotrypsin catalyzed 3 + 7 fragment coupling synthesis with conversion rates of the amino component in the range from 90.3 to 97.4%. For D-Phe6-GnRH the method was scaled up to production level.
通过胰凝乳蛋白酶催化的3 + 7片段偶联合成法制备了D-Xaa6-促性腺激素释放激素类似物(Xaa:丙氨酸、1-萘基丙氨酸)、苯丙氨酸、叔丁基丝氨酸、色氨酸,氨基组分的转化率在90.3%至97.4%之间。对于D-苯丙氨酸6-促性腺激素释放激素,该方法已扩大到生产规模。