METHOD OF SYNTHESIZING THE TRICYCLIC KETONES AND CAPTOTHECIN ANALOGS THEREFROM

摘要

Aprocess for preparing the tricyclic ketonetosynthesize camptothecin analogs, wherein from Compound (k): (wherein TMS is a trimethylsilyl group, andMe is a methyl group.) , or Compound (v) : (v) (wherein TMS is a trimethylsilyl group, andMe is a methyl group.) , Compound (1) : (1) (wherein TMS is a trimethylsilyl group, and Me is a methyl group.) is produced; and from Compound (1) Compound (m): (m) (wherein TMS is a trimethylsilyl group, andMe is a methyl group.) is produced; and from Compound (m) Compound (n): (n) (wherein TMS is a trimethylsilyl group, Me is a methyl group, and Et is an ethyl group.) is produced; and from Compound (n) Compound (o): (o) (wherein TMS is a trimethylsilyl group, Me is a methyl group, and Et is an ethyl group.) is produced; and from Compound (o) Compound (p): (P) (wherein TMS is a trimethylsilyl group, Me is a methyl group, and Et is an ethyl group.) is produced; and from Compound (p) Compound (q): (q) (wherein Me is a methyl group, and Et is an ethyl group.) is produced; and from Compound (q) Compound (r): (r) (wherein Me is a methyl group, Et is an ethyl group, and Pr is a propyl group.) is produced; and from Compound (r) Compound (s): (s) (wherein Et is an ethyl group, and Pr is a propyl group.) is produced; and from Compound (s) Compound (t): (wherein Et is an ethyl group, and tBu is a t-butyl group, is produced; and from Compound (t) Compound (h): (t) (h) (wherein Et is an ethyl group.) is produced, wherein it contains steps: (1) a step to obtain Compound (1) by mixing Compound (k), n-butyl lithium as a lithiating agent, a formylation reagent and an iodination reagent; and one or more steps selected from the group consisting of