一种保护的磷酸氨基酸的一般制备方法。

A general preparation of protected phosphoamino acids.

机构信息

Chemical Process Research and Development, Cephalon Inc., 383 Phoenixville Pike, Malvern, Pennsylvania 19355, USA.

出版信息

Org Lett. 2012 Mar 2;14(5):1206-9. doi: 10.1021/ol203332j. Epub 2012 Feb 22.

DOI:10.1021/ol203332j

Abstract

Fmoc-O-benzyl-l-phosphoserine is an important building block in the synthesis of Forigerimod, a phosphopeptide being investigated for Systemic Lupus Erythematosus (SLE). An efficient one-pot process was developed using inexpensive, readily available starting materials. This general procedure was used to prepare a variety of protected phosphoamino acids.

摘要

芴甲氧羰基-O-苄基-l-磷酸丝氨酸是福瑞格美（一种正在研究用于治疗红斑狼疮的磷酸肽）合成中的重要砌块。使用廉价、易得的起始原料开发了一种高效的一锅法工艺。该通用方法已用于制备各种保护的磷酸氨基酸。