1510832-19-5Relevant articles and documents
Preparation method of Rayleigh bactam intermediate
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Paragraph 0042-0044, (2020/09/12)
The invention discloses a preparation method of a Rayleigh bactam intermediate. (2S, 5R)-5-[(benzyloxy) amino] piperidine-2-formate II is used as a raw material and reacts with Boc-4-aminopiperidine III in the presence of an accelerant to generate 4-((2S, 5R)-((benzyloxy) amino) piperidine-2-formamide) piperidine-1-tert-butyl formate I. The method has the advantages of readily available raw materials, mild reaction conditions, high reaction selectivity, high reaction speed, few impurities and the like.
PREPARATION OF TERT-BUTYL 4-((1R,2S,5R)-6- (BENZYLOXY)-7-0X0-1,6-DIAZABICYCL0[3.2.I]OCTANE-2- CARBOXAMIDO)PIPERIDINE-1-CARBOXYLATE
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, (2015/01/09)
A process for the preparation of N-protected 6-(piperidin-4-ylcarbamoyl)piperidin-3-yl sulfonates of Formula (III): which comprises contacting a lactone of Formula (II): with an azacycloalkylamine of formula (II-Am): followed by contact with a sulfonyl halide of formula (II-Su): R4-SO2W (II-Su) in the presence of tertiary amine base, wherein PG1 and PG2 are amine protective groups; k, p and q are 0, 1, or 2, and W, R2, R3, R4, R5, R6, R7, R8, and R9 are defined herein. Additional embodiments add a series of process steps leading to the synthesis of 7-oxo-1,6-diazabicyclo[3.2.1]octanes suitable for use as β-lactamase inhibitors.