Intermediary compounds for the hemisynthesis of taxanes and prepn. processes therefor

Intermediary compounds for the hemisynthesis of taxanes and prepn. processes therefor

  • CN 1,200,731 A
  • Filed: 10/25/1996
  • Published: 12/02/1998
  • Est. Priority Date: 10/27/1995
  • Status: Abandoned Application
First Claim
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1. the method for preparing the taxanes side chain precursor, wherein in single step, by Ritter reaction the cis of formula I-beta-aromatic glycidic acid ester derivative is transformed, the zone specifically or three-dimensional β

  • -N-alkylamide and Alpha-hydroxy or their cyclic precursor of producing specifically In the formula;

    Ar represents aryl, andR represents alkyl, and preferred straight or branched alkyl or cycloalkyl is replaced by one or several alkyl in case of necessity, and this method comprises;

    A makes formula I cis beta-aromatic glycidic acid ester derivative defined above and formula R in the presence of protonic acid and water 2The nitrile reaction of-CN, R in the formula 2The expression aryl, the beta-aromatic Isoserine derivatives that obtains general formula I Ia comes direct synthesizing linear chain Ar, R and R in the formula 2Define as the front;

    Perhaps B in anhydrous medium, makes formula I cis beta-aromatic glycidic acid ester derivative defined above and formula R '"'"' in the presence of Lewis acid or protonic acid 2The nitrile of-CN reacts, the R '"'"' in the formula 2Expression R as defined above 2, perhaps low alkyl group, perhaps rudimentary whole haloalkyl such as trichloromethyl, obtains formula IIb De oxazoline, and direct synthesis of cyclic chain, Ar, R and R '"'"' in the formula 2Define as the front.

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