To obtain the subject new vitamin D3 analogue or derivative having a biologically calcium-controlling action and a tumor cell differentiation-inducing action.
An vitamin D3 analogue of formula I (R1 is H and R2 is OH, or R1 is OH and R2 is H; R3 is an OH-protecting group; R5 and X are each H or the like). For example, a compound of formula II. The compound is effectively obtained by coupling (A) a new fluorine-containing alicyclic compound of formula III with (B) a phosphine oxide of formula IV (R6 is an alkyl or the like) in an amount of 1-2 equivalents based on the component A in the presence of a base (an alkyl lithium or the like) at -100 to 50°C in an inactive gas atmosphere in an ether solvent for 10 min to 24 hr. The removal of at least the 25-protecting group in the compound of formula I to form an OH group enables to obtain a fluorine-containing vitamin D3 analogue whose excellent pharmacological activity has been known.
ASADA DAISUKE
KUROKI KATSUCHIKA
| JPS5886146A | 1983-05-23 | |||
| JPS61220591A | 1986-09-30 | |||
| JPS5884110U | 1983-06-07 | |||
| JPS6222638A | 1987-01-30 |