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An Improved, Practical, and Scalable Five-Step Synthesis of Psilocybin
Synthesis ( IF 2.2 ) Pub Date : 2020-01-08 , DOI: 10.1055/s-0039-1691565
Alexander M. Sherwood , Poncho Meisenheimer , Gary Tarpley , Robert B. Kargbo

Described herein is an improved synthesis of 3-[2-(dimethylamino)ethyl]-1H-indol-4-yl dihydrogen phosphate (psilocybin). The protocol outlines: synthesis of multigram quantities of psilocybin, identification of critical in-process parameters, and isolation of psilocybin without the use of chromatography, TLC, or aqueous workup. The synthesis furnishes psilocybin in five steps in 23% overall yield from an inexpensive acetoxyindole starting material. With specific focus on process control and impurity fate and removal, the improved procedure is amenable to providing high-quality psilocybin.

中文翻译:

改良的,实用的和可扩展的五步合成胞菌素

本文描述了3- [2-(二甲基氨基)乙基] -1 H-吲哚-4-基磷酸二氢盐(psilocybin)的改进的合成。该协议概述:合成数克量的psilocybin,鉴定关键的工艺参数以及在不使用色谱,TLC或水处理的情况下分离psilocybin。该合成可从便宜的乙酰氧基吲哚原料中分五步以总产率23%的方式提供psilocybin。特别关注过程控制以及杂质去向和去除,改进后的程序适用于提供高质量的梭菌酶。
更新日期:2020-01-09
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