Process for preparing 2.alpha.-methyl-2.beta.-(1,2,3-triazol-1-y

Organic compounds -- part of the class 532-570 series – Organic compounds – Heterocyclic carbon compounds containing a hetero ring...

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C07D49900, A61K 31425

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048959413

ABSTRACT:
2.alpha.-Methyl-2.beta.-(1,2,3-triazol-1-yl)methylpenam-3.alpha.-carboxylic acid derivatives are prepared by reacting a penicillanic acid sulfoxide derivative of the formula ##STR1## wherein R is a penicillin carboxyl protecting group, and R.sub.1 is hydrogen or halogen, R.sub.2 is hydrogen, lower alkyl or the like with a triazole derivative of the formula ##STR2## wherein R.sub.3 and R.sub.4 are hydrogen, trialkylsilyl, lower alkyl, lower alkoxy or the like and R.sub.5 is hydrogen or silyl substituted with 3 groups selected from the class consisting of lower alkyl, benzyl and phenyl in a solvent.

REFERENCES:
patent: 4496484 (1985-01-01), Micetich et al.
patent: 4529592 (1985-07-01), Micetich et al.
patent: 4562073 (1985-12-01), Micetich et al.
patent: 4668514 (1987-05-01), Micetich et al.
patent: 4774238 (1988-09-01), Broom et al.
Tetrahedron Letters No. 38, pp. 3303-3306 (1975).
Micetich et al., Synthesis 1986, 292 published Apr., 1986.

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