3-hydroxy-N-methylpyrrolidone and use as transdermal enhancer

Drug – bio-affecting and body treating compositions – Preparations characterized by special physical form – Web – sheet or filament bases; compositions of bandages; or...

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424449, 514946, 514947, A61F 1302

Patent

active

050324020

ABSTRACT:
The novel compound, 3-hydroxy-N-methylpyrrolidone, is effective as a transdermal enhancer for the absorption of drugs through the skin of humans and animals. The 3-hydroxy-N-methylpyrrolidone is prepared from delta-butyrolactone which is converted to methyl 2,4-dibromobutyrate, this intermediate is reacted with methylamine to form N-methyl-2,4-dibromobutyramide, this intermediate is converted to 3-bromo-N-methyl-2-pyrrolidone by ring closure, and the 3-bromo-N-methyl-2-pyrrolidone is reacted with an alkaline earth metal carbonate or alkaline metal carbonate to form 3-hydroxy-N-methyl-2-pyrrolidone.

REFERENCES:
patent: 4039664 (1977-08-01), Stoughton
patent: 4537776 (1985-08-01), Cooper
patent: 4568343 (1986-02-01), Leeper

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