Department of Chemistry, Indian Institute of Technology Bombay, Powai, Mumbai-400076, India.
Org Biomol Chem. 2020 Apr 1;18(13):2432-2446. doi: 10.1039/d0ob00170h.
This work reports the construction of key building blocks towards the synthesis of cortistatins; a family of steroidal alkaloids. Cortistatin A, being a primary target due to its superior biological properties over other congeners, has been prepared by two different synthetic routes. Synthesis of the precursor to the heavily substituted A-ring starting from d-glucose and construction of the DE-ring junction employing a Hajos-Parrish ketone as a chiral pool have been demonstrated. Efforts are underway to assemble these key fragments and build towards the total synthesis of cortistatin A.
这项工作报道了关键砌块的构建，用于合成甾体生物碱 cortistatins；其中 cortistatin A 因其优于其他同系物的优异生物特性而成为主要目标，已通过两种不同的合成路线制备。已经证明，从 d-葡萄糖开始合成 A 环的前体，并使用 Hajos-Parrish 酮作为手性池构建 DE-环连接。正在努力组装这些关键片段，以构建 cortistatin A 的全合成。
