# TOTAL SYNTHESIS OF CATHARANTHINE & ANTICANCER ALKALOIDS

> **NIH NIH R01** · UNIVERSITY OF WASHINGTON · 1989 · $99,138

## Abstract

The dimeric Catharanthus alkaloids vinblastine and vincristine are
extremely efficacious, clinically useful anticancer agents.  The isolation
and purification of these compounds is a difficult process.  The use of
these compounds for cancer chemotherapy often causes serious side effects.
The desirability of preparing and testing analogs of these compounds is
apparent.

Semisynthetic vinblastine and vincristine have been prepared by the
coupling of naturally occurring vindoline and catharanthine.  This approach
has several significant limitations.  Although vindoline is readily
available from natural sources, catharanthine is relatively
inaccessibility.  In addition, the coupling procedure is not very
efficient.  Finally, the use of naturally obtained vindoline and
catharanthine restricts the types of dimeric analogs which may be prepared.

The objective is to develop efficient methods for the preparation of the
dimeric Catharanthus alkaloids vinblastine and vincristine, and analogs of
these compounds.  The specific aims are:  (1) to develop improved
procedures for the coupling of synthetic (=)-catharanthine with
(+)-vindoline in order to prepare the dimeric alkaloids; (2) to prepare
analogs of catharanthine; and (3) to prepare a large number of dimeric
alkaloid analogs, which will be submitted for testing of biological
activity.

## Key facts

- **NIH application ID:** 3170873
- **Project number:** 5R01CA032976-06
- **Recipient organization:** UNIVERSITY OF WASHINGTON
- **SAM.gov UEI:** HD1WMN6945W6
- **Principal Investigator:** STANLEY RAUCHER
- **Activity code:** R01 (R01, R21, SBIR, etc.)
- **Funding institute:** NIH
- **Fiscal year:** 1989
- **Award amount:** $99,138
- **Award type:** 5
- **Project period:** 1982-07-01 → 1990-11-30

## Primary source

NIH RePORTER: https://reporter.nih.gov/project-details/3170873

## Citation

> US National Institutes of Health, RePORTER application 3170873, TOTAL SYNTHESIS OF CATHARANTHINE & ANTICANCER ALKALOIDS (5R01CA032976-06). Retrieved via MORVS 2026-10-25 from https://api.morvs.ai/grant/nih/3170873. Licensed CC0.

---

*[NIH grants dataset](/datasets/nih-grants) · CC0 1.0*