Patent · US Expired

14-halo-camptothecins

US5459269A · kind A · utility

6Cited by
7References
8Claims
0Family size

Assignee

Inventor

Key dates

Filing dateDec 2, 1994
Grant dateOct 17, 1995
Priority date
Expiry dateDec 2, 2014

Classification

  • Technology area (CPC C)Chemistry; Metallurgy
  • CPC primaryC07D491/04
  • WIPO fieldOrganic fine chemistry
  • WIPO sectorChemistry

Abstract

A method of making racemic DE ring intermediates for the synthesis of camptothecin and camptothecin analogs employing novel intermediates of Formula (XX) and (XXI): ##STR1## wherein R.sub.20 is loweralkyl, R is loweralkyl, Y is H or halogen, and R.sub.21 is loweralkoxy; as precursors to the DE ring intermediate. The present invention also provides a camptothecin analog of Formula (I-A): ##STR2## wherein: Hal is a halogen; PA1 and the remainder of the variables are as defined in the specification. Additionally, other novel compounds useful in the preparation of the compounds of Formula (I-A) and methods of producing compounds of (I-A) are also provided.

Source: USPTO / EPO open patent data. Objective bibliographic and citation counts.