脱水環化試薬を使用するＮ−オキシドのＮ−脱メチル化によるモルヒネ類似体の調製における方法および中間体

摘要

A compound of Formula V
wherein ---- represents a single or double bond, provided that two double bonds are not adjacent to each other;
R 1 and R 2 are independently selected from C 1-10 alkyl, C 6-10 aryl, C 3-10 cycloalkyl, C 1-10 alkyleneC 6-10 aryl, C 1-10 alkyleneC 3-10 cycloalkyl and PG, except when - - O represents =O, then R 2 is not present;
PG is a protecting group;
R 3 is selected from C 3-10 cycloalkyl, C 3-10 cycloalkenyl, C 1-10 alkyl, C 2-10 alkenyl, C 6-10 aryl, C 1-10 alkyleneC 6-10 aryl and C 1-10 alkyleneC 3-10 cycloalkyl;
X is a counteranion, and
one or more available hydrogens in R 1 , R 2 and R 3 is/are optionally replaced with F and/or one or more of available atoms in R 1 , R 2 and R 3 is/are optionally replaced with an isotopic label,
or a salt or solvate thereof.