Process for preparation of cytostatic compounds
US4410459A · kind A · utility
Assignee
Inventors
Key dates
| Filing date | Aug 17, 1981 |
| Grant date | Oct 18, 1983 |
| Priority date | — |
| Expiry date | Aug 17, 2001 |
Classification
- Technology area (CPC A)Human Necessities
- CPC primaryA61P35/00
- WIPO fieldOrganic fine chemistry
- WIPO sectorChemistry
Abstract
The invention relates to new cytostatic compound, process for their preparation and pharmaceutical compositions containing them. More particularly, there are provided new compounds of the general formula ##STR1## in which R.sup.4 is .beta.-hydroxyl and PA1 R.sup.3 is .alpha.-ethyl; or PA1 R.sup.4 is hydrogen and PA1 R.sup.3 is .beta.-ethyl; PA1 R" is a straight chained alkyl having from 1 to 10 carbon atoms, or a branched chained alkyl having from 3 to 10 carbon atoms, in which groups the carbon atom attached to the >N.sub.a -CH.sub.2 -O-- group has a primary or secondary configuration or an alkenyl or alkinyl having from 3 to 6 carbon atoms, or an aralkyl having from 1 to 3 carbon atoms in the alkyl moiety; PA1 R.sup.1 is methoxy and PA1 R.sup.2 is acetyl, PA1 provided that if R.sup.3 is .alpha.-ethyl and R.sup.4 .beta.-hydroxyl, R.sup.4 is other than ethyl. These compounds and N-desmethyl-N- ethoxy- methyl -vinblastine can be prepared according to the invention by transetherification of compounds of the compounds of the general formula ##STR2## with a large excess of alcohols of the general formula EQU R"--OH (III) Pharmaceutical compositions containing compounds of the general f…
Source: USPTO / EPO open patent data. Objective bibliographic and citation counts.