苔蘚蟲素化合物及其製備方法农业专利-农业学术服务平台

发明人:: WENDER, PAUL,温德　保罗,溫德　保羅,QUIROZ, RYAN,克罗姿　雷恩,克羅姿　雷恩,HO, STEPHEN,何　史蒂芬,SHIMIZU, AKIRA,清水　亮,RYCKBOSCH, STEVEN,雷克博斯　史蒂芬,STEVENS, MATTHEW C.,史蒂芬斯　马修,史蒂芬斯　馬修,JEFFREYS, MATTHEW S.,杰佛瑞　马修,温德保罗,溫德保羅,克罗姿雷恩,克羅姿雷恩,何史蒂芬,清水亮,雷克博斯史蒂芬,史蒂芬斯马修,史蒂芬斯馬修,杰佛瑞马修

摘要：: Methods for preparing a variety of bryostatin compounds are provided. The subject methods provide for preparation of bryostatin 1 in multi-gram quantities in a low and unprecedented number of convergent synthetic steps from commercially available materials. The subject methods are scalable with low estimated material costs and can provide enough material to meet clinical needs. Also provided are a variety of bryostatin analog compounds, and prodrug forms thereof, which are synthetically accessible via the subject methods and pharmaceutical compositions including the same.提供用於製備多種苔蘚蟲素化合物的方法。該等標的方法提供由可商購的材料以少且無先例的數目的收斂式合成步驟製備以數公克量的苔蘚蟲素1。該等標的方法可在估計材料成本低的情況下規模化且可提供足夠的材料以滿足臨床需要。亦提供可經由該等標的方法合成獲得的多種苔蘚蟲素類似物化合物及其前藥形式以及包括其之醫藥組成物。