专利号:US-5132419-A 优先权日:1989-10-03 标题 :Process for the preparation of 7-amino-3-((z)-1-propen-1yl)-3-cephem-4-carboxylic acid 发明人:LANZ JOACHIM; NAAB PAUL; ROSENTRETER ULRICH 权利人:BAYER AG 摘要:(7-APCA) having the formula (I) ##STR1## which is an important synthesis intermediate in the preparation of cephalosporin-like antibiotics, is prepared by treating a compound of the formula (II) ##STR2## in which R 1 and R 2 represent alkyl, aryl and aralkyl radicals, with a strong protonic acid or with a Lewis acid. Compound (II) is prepared by adding triphenylphosphine and alkali metal iodide to a compound of the formula (VI) ##STR3## then reacting with acetaldehyde in base. Compound (VI) is prepared by treating a compound of the formula (VII) ##STR4## with a base in a polar solvent at -70° C. to 0° C. Compound (VII) is prepared by treating a compound of the formula (VIII) ##STR5## with a chlorinating agent in an organic solvent.
专利号:WO-2010082108-A1 优先权日:2009-01-16 标题:Improved process for preparation of key intermediate of cephalosporins 发明人:SAHOO PRABHAT KUMAR; SHRIVASTAVA AJAY KUMAR; YADAV CHHANNU LAL; CHAUBEY BIPIN KUMAR 权利人:NECTAR LIFESCIENCES LTD; SAHOO PRABHAT KUMAR; SHRIVASTAVA AJAY KUMAR; YADAV CHHANNU LAL; CHAUBEY BIPIN KUMAR 摘要:An improved process for the preparation of 7-phenylacetamido-3-vinyl cephalosporanic acid-p-methoxybenzyl ester of formula (I), which is a key intermediate of cephalosporin antibiotics and is extremely useful in their synthesis, is provided. More particularly, an improved process for the preparation of a compound of formula (I) by using a compound of formula (A) is provided, wherein, R represents hydrogen, alkyl, aryl or arylalkyl, which may be same or different and may be further substituted, making it a substantially cost effective and eco-friendly procedure.
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