F. Kajfez

CHIRAL 1,4‐BENZODIAZEPINES PART 5, SYNTHESIS AND PROPERTIES OF 1,4‐BENZODIAZEPIN‐2‐ONES CONTAINING ALPHA‐AMINO ACIDS AS A PART OF THE 1,4‐DIAZEPINE RING

Chiral 1,4-benzodiazepin-2-ones XIII-XXIIII (Scheme 1) were prepared starting from N-protected α-amino acids and 2-amino-5chlorobenzeophenone; the intermediates I-XII were isolated and identified. Spectroscopie propertiec of these componds are discussed (ir, nmr); their optical stability, as well as the cyclization rate for XII-XIII in buffer solution have been determined.

SYNTHESEN VON EINIGEN PHARMAKOLOGISCH UND STEREOCHEMISCH INTERESSANTEN DERIVATEN DER CAMPHANSAEURE

Das aus Camphansaure (I) auf ublichem Wege dargestellte Amid (II) wird mit POCl3 zum Nitril (III) dehydratisiert; eine Reaktion dieses Nitrils mit H2S in Pyridin-Tri- athylamin liefert das Thioamid (IV).