- Synthesis method of Avibactam intermediate
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The invention discloses a synthesis method of an Avibactam intermediate, and belongs to the technical field of the medicine chemical synthesis. The synthesis method comprises the following steps: reacting pyroglutamate containing an amino protecting group with trimethylsulfoxonium iodide in a reaction solvent under the effect of the carbonate to obtain the Avibactam intermediate. The problems thata strong alkali process method in the prior art is large in potential safety hazard, relatively difficult in process control and high in impurity content are avoided, and the synthesis method disclosed by the invention is mild in reaction condition, simple in operation, high in process operability security, high in yield, high in product purity and suitable for the industrial production.
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Paragraph 0044-0046
(2018/11/27)
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- PREPARATION OF ALKYL ESTERS OF N-PROTECTED OXO-AZACYCLOALKYLCARBOXYLIC ACIDS
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A process for the preparation of alkyl esters of N-protected oxo-azacycloalkylcarboxylic acids of Formula III: comprises contacting a ketosulfoxonium ylide of Formula II: with an iridium catalyst to obtain Compound III, wherein PG1 is an amine protective group group; k is 0, 1, or 2; and RU, R1, R2, and R3 are defined herein. An embodiment of the process further com rises contacting a compound of Formula I: with a sulfoxonium halide of formula (RU)3S(O)Z, wherein Z is halide, in the presence of a strong base to obtain Compound II. 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.
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Page/Page column 29
(2010/11/17)
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