Thioamides

C - Chemistry – Metallurgy – 07 – D

Patent

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260/336

C07D 205/08 (2006.01)

Patent

CA 1051008

A B S T R A C T The invention relates to compounds of the formula: Image 1 wherein R stands for lower alkyl, aryl, heteroaryl, benzyl, heteroarylloweralkyl, phenoxyloweralkyl, phenylthio- loweralkyl, 4-amino-1-butyl and suitably protected derivatives, .alpha.-aminobenzyl and protected derivatives such as the carbamates (benzyl, trichloroethyl and methoxymethyl) and aldehyde and ketone adducts, .alpha.- hydroxybenzyl and protected derivatives, .alpha.-carboxy- benzyl and protected derivatives, .alpha.-sulfobenzyl and protected derivatives, the radical R5O-, R5S, or R5R6N-, wherein R5 and R6 may be the same or different and each be taken from the group lower alkyl, aryl, arylloweralkyl and heteroaryl and additionally, in the case of R5R6N-, R5 and/or R6 may be hydrogen; R1 is hydrogen or a cleavable radical such as lower- alkoxymethyl, acyloxymethyl, loweralkylthiomethyl, loweralkyl, 2,2,2-trichloroethyl, benzyl, substi- tuted (nitro, methoxy or halo) benzyl, benzhydryl, phenacyl or trialkylsilyl; R2 is hydrogen or methoxy; R3 stands for lower alkyl, aryl, arylloweralkyl, heteroaryl, and the radicals R5O-, R5S-, R5R6N-, or R5R6NR7N- wherein R5 and R6 have the same meaning set forth above; and R7 has the same meaning as R5 or R6 including hydrogen, and R4 has the same meaning as R5 or R6 including hydrogen. The novel compounds are useful intermediates in the preparation of cephalosporins and penicillins.

229977

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