8-chloro-2,3-benzodiazepine derivatives

A process for the preparation of a compound of the formula (I)

• wherein
• R is a C1 to C6 alkyl group or —NHR1, wherein
• R1 is a C1 to C6 alkyl or a C3 to C7 cycloalkyl group, or a pharmaceutically acceptable acid addition salt thereof, which comprises
• (a) reducing a compound of the formula (II),
• wherein R is as stated above;
• or
• for the preparation of a compound of the formula (I)
• wherein R is specifically —NHR1 wherein R1 is as stated above,
• (b) reacting a compound of the formula (IV),
• wherein Y is a lower alkyl group or a leaving group, with a compound of the formula (V),
• H2N—R1 (V)
• wherein R1 is as stated above, and, if desired, converting the compound of the formula (I) thus obtained into a pharmaceutically acceptable acid addition salt thereof.

A process for the preparation of a compound of the formula (II)

• wherein
• R is a lower alkyl group or —NHR1, wherein
• R1 is a lower alkyl or a lower cycloalkyl group , or a pharmaceutically acceptable acid addition salt thereof, which comprises the steps of:
• reacting a compound of the formula (VII)
• with a reagent capable of introducing a Y group, and reacting the thus-obtained compound of the formula (VIII)
• with a compound of the formula (V)
• H2N—R1 (V)
• to obtain the desired product.