| 摘要 |
The present invention relates to a method of making compounds of Formula V
wherein part of the synthesis comprises reducing a compound of Formula VI to a compound of Formula VII in the presence of Baker's yeast
wherein the dashed lines indicate the presence or absence of a bond, the hatched wedges indicate the ±(down) configuration, and the solid triangles indicate the ²(up) configuration;
B is a single, double, or triple covalent bond;
n is 0-6;
X is CH 2 , S or O;
Y is any pharmaceutically acceptable salt of CO 2 H, CO 2 R, CONR 2 , CONHCH 2 CH 2 OH, CON(CH 2 CH 2 OH) 2 , CH 2 OR, P(O)(OR) 2 , CONRSO 2 R, SONR 2 , or
R is H, C 1-6 alkyl or C 2-6 alkenyl;
R 2 and R 3 are C 1-6 linear alkyl which may be the same or different, and may be bonded to each other such that they form a ring incorporating the carbon to which they are commonly attached;
R 5 is hydrogen or R; and
R 6 is
i) hydrogen;
ii) a linear or branched hydrocarbon containing between 1 and 8 carbon atoms, which may contain one or more double or triple bonds, or oxygen or halogen derivatives of said hydrocarbon, wherein 1-3 carbon or hydrogen atoms may be substituted by O or a halogen; or
iii) aryloxy, heteroaryloxy, C 3-8 cycloalkyloxy, C 3-8 cycloalkyl, C 6-10 aryl or C 3-10 heteroaryl, wherein one or more carbons is substituted with N, O, or S; and which may contain one or more substituents selected from the group consisting of halogen, trihalomethyl, cyano, nitro, amino, hydroxy, C 6-10 aryl, C 3-10 heteroaryl, aryloxy, heteroaryloxy, C 1-6 alkyl, OR, SR, and SO 2 R. |
