Industrial process for the preparation of (1S)-1-[N-(4-O-deacety

Details Industrial process for the preparation of (1S)-1-[N-(4-O-deacety Industrial process for the preparation of (1S)-1-[N-(4-O-deacety

1991-03-25

1992-09-22

Rotman, Alan L.

Organic compounds -- part of the class 532-570 series

Organic compounds

Heterocyclic carbon compounds containing a hetero ring...

C07F 965, C07F 9576, C07F 959

Patent

active

051498120

ABSTRACT:
Industrial synthesis of (1S)-1-[N-(4-O-deacetyl-23-vinblastinoyl)amino]-2-methylpropyl diethyl phosphonate and its salts by condensation of 4-O-deacetylvinblastinoic acid (obtained by alkaline hydrolysis of vinblastine sulphate) with phosamine (+) (dextrorotatory isomer of 1-amino-2-methylpropyl diethyl phosphonate), by means of BOP, a peptide coupling reagent, [1-benzotriazolyloxytris(dimethylamino)phosphonium hexafluorophosphonate]; and, if desired, the product obtained is converted into a salt with suitable acids.

REFERENCES:
Chemical Abstracts, vol. 113(11) Abstract No. 113:91020-x Sep. 10, 1990.
Chemical Abstracts, vol. 112(25) abst. No. 112:235,666s Jun. 18, 1990.
Anticancer Research 10: 139-144 (1990).
The Journal of Medicinal Chemistry, 34, No. 7, (1991), pp. 1998-1999.

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