Imidazole derivatives, process for production thereof, and use t

Details Imidazole derivatives, process for production thereof, and use t Imidazole derivatives, process for production thereof, and use t

1989-02-28

1991-10-22

Kilby Scalzo, Catherine S.

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Carbohydrate doai

514397, 536 11, 536 187, 548110, 548116, 548336, A61K 3170, C07H 504, C07D23366

Patent

active

050595903

ABSTRACT:
Disclosed are imidazole derivatives represented by formula [I]: ##STR1## wherein R is a hydrogen atom or ##STR2## wherein R.sup.2 is a hydrogen atom or a hydroxy protecting group, R.sup.2 protecting either a single hydroxy or two hydroxies together when R.sup.2 is a hydroxy protecting group, and R.sup.3 is a hydrogen atom or OR.sup.2 ; A is CONH.sub.2 or CN; and R.sup.1 is a hydrogen atom, lower alkyl, hydroxy lower alkyl, or phenyl.
Also disclosed are six processes for producing these novel compounds among which a typical process comprises reacting a starting imidazole compound having a halogen at the 5-position thereof with an acetylene derivative to alkynylate the 5-position.
Furthermore, the compounds having remarkable antitumor activities and therefore can provide novel antitumor agents.

REFERENCES:
patent: 4144347 (1979-03-01), Stern
patent: 4594353 (1986-06-01), Colle et al.

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