Organic Chemistry of Drug Synthesis. Volume 7

(Brent) #1

(DBU) flowed by methyl iodide leads to the corresponding methyl ester 11.
Heating 11 with ethylamine leads to ester interchange and formation of the
ethyl amidebimatoprost( 12 ).^4


HO

OH OH

CO 2 H

10

HO

OH OH

CO 2 CH 3

11

HO

OH OH

CO 2 NHC 2 H 5

12

DBU
CH 3 I

C 2 H 5 NH 2

A PGE related compound,lubiprostone( 23 ) displays a quite different
spectrum of activity. This compound has been recently approved for treat-
ment of chronic constipation and is being investigated for its effect on
constipation-predominant irritable bowel syndrome. It has been ascertained
that the drug interacts with specific ion channels in the GI tract causing
increased fluid output into the lumen. Starting material for the synthesis
( 13 ) comprises yet another variant on the Corey lactone. Condensation


O

O

THPO CH=O
13

+
O

F F
P
O

HH 33 CCOO

O

O

THPO O

F F

14 15

O

O

THPO O

F F

16

H 2
O

O

THPO OH

F F

17

O

OH

THPO O

F F

18

DiBAL NaBH 4

(C 6 H 5 ) 3 P+(CH 2 ) 3 CO 2 –

OH

THPO O


F

19

F

CO 2 H

OH

THPO O

F
20

F

CO 2 CH 2 C 6 H 5 1. CrO^3


  1. AcOH


O

HO O

F
21

F

CO 2 CH 2 C 6 H 5

O

HO O

FF

H 2
CO 2 H

O

FF

CO 2 H

22

O
HO
23

tBuOK

24 ALICYCLIC COMPOUNDS

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