Andersen N H, Imamoto S, Picker D H
Prostaglandins. 1977 Jul;14(1):61-101. doi: 10.1016/0090-6980(77)90157-5.
With the report given herein all diastereomers of PGF2, PGE2, and PGD2 which bear the naturally recognized 15-S hydroxylated center, whether in the natural or entprostanoic acid skeleton, have been prepared by a route involving initial introduction of the carboxyl (alpha) chain (1). A major advantage of the initial alpha-ylation route is the facile reduction of the 13, 14-en-15-one system with methanolic NaBH4 which proceeds without competing 1,4-reduction. The products are thus free of 13,14-dihydro-PG2 contaminants (2). The initial pharmacological evaluation of these diastereomers will be submitted for publication in this journal (3).
根据本文给出的报告，所有带有天然公认的15 - S羟基化中心的PGF2、PGE2和PGD2非对映异构体，无论其处于天然或内前列腺素酸骨架中，均已通过一种涉及首先引入羧基（α）链的路线制备出来（1）。最初的α - 酰化路线的一个主要优点是，用甲醇钠硼氢化物对13,14 - 烯 - 15 - 酮体系进行还原很容易，且该过程不会发生竞争性的1,4 - 还原。因此，产物中不含13,14 - 二氢 - PG2污染物（2）。这些非对映异构体的初步药理学评估将提交至本期刊发表（3）。
