| 摘要 |
<p>1506518 Tetrazolylpenam derivatives PFIZER Inc 27 Nov 1975 [29 Nov 1974] 48886/75 Heading C2C [Also in Division C3] Novel penam compounds of the formula wherein R is a hydrogen atom, C 1-12 alkyl, C 3-7 cycloalkyl, phenyl, substituted phenyl, naphthyl, substituted naphthyl, furyl, thienyl or pyridyl, or C 2-12 alkenyl, each substituted group containing one or two substituents, each of which is a Cl, Br, I, OH, NO 2 , C 1-4 alkoxy or C 1-4 alkyl ; Y is a group of the formula wherein R 1 is R 2 or a tetrazolylpenam nitrogen protecting group, R 2 is H, C 3-8 alkanoyloxymethyl, C 4-9 alkanyloxyethyl, silyl, phthalidyl or a group of the formula wherein each of R 4 , R 5 and R 6 is H, Cl, Br, F, C 1-4 alkyl, C 1-4 alkoxy, or phenyl, and salts of those compounds wherein R 1 and R 2 are H atoms may be prepared by reacting an optionally R 1 or R 2 substituted 6-amino-2,2-dimethyl- 3-(5-tetrazolyl)penam with an aldehyde of the formula RCHO. A 6-acylamino-2,2-dimethyl-3(5-tetrazolyl)- penam is obtained by acylating an imine of Formula III with a compound of Formula R 3 COX to form an imine of Formula (IV) and hydrolysing the imine to form the product of Formula (V) Detailed preparations of intermediates (I) via the corresponding 6 - triphenylamino - 2,2- dimethyl - 3(5 - tetrazolyl)penams is also described.</p> |
