| 主权项 |
1. A process for the preparation of a compound of formula (I): wherein: the dotted line denotes a bond which is single or double,
R1 and R′1 are the same or different and represent H or CH3,R2 is H, CH3 or C2H5,R3 is —NRR′ wherein R and R′ are the same or different and are selected from the group consisting of: —H, —(CH2)n-OH wherein
n is an integer comprised between 1 and 4, —(CH2)n-NHP wherein
n is an integer comprised between 1 and 6 andP is H or a protecting group; —(CH2)n-NP—(CH2)m-NHP′ wherein
n is an integer comprised between 1 and 6,m is an integer comprised between 1 and 6, andP and P′ are the same or different and represent H or a protecting group; —(CH2)n-NP—(CH2)m-NP′—(CH2)p-NHP″ wherein
n is an integer comprised between 1 and 6,m is an integer comprised between 1 and 6,p is an integer comprised between 1 and 6, andP, P′ and P″ are the same or different and represent H or a protecting group; —(CH2)n-X wherein
n is an integer comprised between 1 and 4 andX=imidazol, indol or phenyl, optionally substituted with one or several groups selected from the group consisting of OH, NH2 and SH; R4 is OH, acetoxy or butoxy, said process comprising: (a) reacting an α-epoxy compound of formula (II): wherein R1, R′1, R2, and R4 have the same meaning as in formula (I) and the dotted line denotes a bond which is single or double, with a monoamine or polyamine of formula (III):
R3H (III) wherein R3 has the same meaning as in formula (I) in a reaction medium at reflux; (b) recovering compound (I) from the reaction medium; wherein a 3 to 5 carbon atom alcohol or a mixture of 3 to 5 carbon atom alcohols is used as a solvent in the reaction medium. |
