| 摘要 |
<P>PROBLEM TO BE SOLVED: To provide a novel method of producing prostamide. <P>SOLUTION: The method of producing prostamide includes the steps of: (a) generating a second intermediate represented by Formula (II) by a reaction between a first intermediate represented by Formula (I) and DIBAL; (b) generating a third intermediate by a reaction between the second intermediate and Na(TMS)<SB POS="POST">2</SB>N and (C<SB POS="POST">6</SB>H<SB POS="POST">5</SB>)<SB POS="POST">3</SB>P<SP POS="POST">+</SP>(CH<SB POS="POST">2</SB>)<SB POS="POST">6</SB>CONR<SB POS="POST">2</SB>X<SP POS="POST">-</SP>[in the formula, R is C<SB POS="POST">1-5</SB>alkyl or hydrogen, and X<SP POS="POST">-</SP>is an anion]; (c) forming a fourth intermediate protecting a hydroxyl group by a reaction between the third intermediate and a protective agent; and (d) generating prostamide by removing the protective group.[In the formula, Z is the protective group, and a broken line represents presence or absence of a double bond]. <P>COPYRIGHT: (C)2013,JPO&INPIT |
