| 摘要 |
N-Formyl-S-aralkyl-cysteines, which are intermediates for optically active cysteines (esp. penicillamine), are prepd. in a 'one-pot' reaction in which an isocyanoacetic acid ester, a metallating agent and a carbonyl cpd. are allowed to react at -80 to +80 degrees C (pref. -70 degrees to +40 degrees C) for 2-60 (pref. 5-20) mins., a molar proportion or an excess of an aralkyl mercaptan is added at 0-100 degrees C, and the reaction soln. is worked up in a conventional manner by hydrolysis and saponification to give the N-formyl-S-aralkyl-cysteine. This simple, one-stage process enables the products to be produced cheaply on a large scale.
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