Prepn. of 6H-ergoline derivs. - by cyanamide cleavage of corresp. 6-cyano cpd. using metallo:organic cpds.

摘要

The prepn. of 6-H-ergoline derivs of formula (I) comprises reacting a 6-cyano-ergoline deriv. of formula (II) with a metallorganic cpd. In the formulae R1 = H, 1-6C alkyl or aryl sulphonyl; R2 = H, 1-6C alkyl, 2-6C alkenyl, Ch2O-(1-4C)alkyl, CH2S-(1-4C)alkyl or Ch2OH; R8 = alpha-NHCXNEt2 or beta-CH2Y X= O or S; Y = H, OH, S-(1-4C)alkyl or O-(1-4C)alkyl; or represents a single or double bond, providing that, if R8 = beta-CH2Y, Ca-C10 is not a double bond. USE/ADVANTAGE - (I) are intermediates for pharmaceuticals contg. alkyl, alkenyl or cycloalkyl alkyl gps in the 6-position. Cyanamide cleavage with the metallorganic cpds. can take place under conditions that do not effect sensitive substits and double bonds, thus retaining the structure and producing a cpd. (I) suitable for N-alkylation to the pharmaceutically active cpds. (K) is produced simply and in good yield without the need for complex sepn. operations.