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houlu666

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Here  we  wish  to  report  a  convenient  alternative synthesis  of  the  diazospiro  system  by  adding  trimethysilyl cyanide  to  (1a) in the  presence  of  catalytic  amounts  of  zinc iodide to  give  the  adduct 2iodide to  give  the  adduct  (2£©(7,8),  which  was  reduced  with LAH to give the amino alcohol (3), and subsequently ring closed with  triphosgene  to  give  the  desired  compound  (4a)  in 72% yield  from  (3). Using the same technique we  also converted 1- (2-phenylethyl)-4-piperidone  (1b) to  Fenspiride  (4b),a bronchodilator  blocker  (9,10).

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