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Details for Patent: 4,824,968

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Details for Patent: 4,824,968

Title: Substituted aromatic sulfonamides as antiglaucoma agents
Abstract:Aromatic sulfonamides with a saturated heterocycle fused thereto are carbonic anhydrase inhibitors useful in the treatment of elevated intraocular pressure.
Inventor(s): Ponticello; Gerald S. (Lansdale, PA), Wiggins; J. Mark (Perkasie, PA)
Assignee: Merck & Co., Inc. (Rayway, NJ)
Filing Date:Jun 26, 1987
Application Number:07/067,332
Claims:1. A process for the preparation of a compound of structural formula: ##STR28## wherein R.sup.14 is

(a) hydrogen,

(b) --CN,

(c) phenyl--C.sub.1-3 alkyl, wherein the phenyl is either unsubstituted or substituted with one or more of

(1) hydroxy,

(2) C.sub.1-3 alkoxy,

(3) R.sup.17 R.sup.18 N--C.sub.1-5 alkyl, wherein R.sup.17 and R.sup.18 are independently selected from:

(i) hydrogen or

(ii) C.sub.1-3 alkyl, or taken together with the nitrogen to which they are attached from a heterocycle selected from morpholine, piperidine pyrrolidine and piperazine;

R.sup.15 is

(a) hydrogen,

(b) C.sub.1-5 alkyl,

(c) phenyl--C.sub.1-3 alkyl, wherein the phenyl is either unsubstituted or substituted with one or more of:

(1) hydroxy,

(2) C.sub.1-3 alkoxy,

(3) R.sup.17 R.sup.18 N--C.sub.1-3 alkyl;

(d) phenyl either unsubstituted or substituted with one or more of

(1) hydroxy,

(2) C.sub.1-3 alkoxy,

(3) R.sup.17 R.sup.18 N--C.sub.1-3 alkyl, or

(4) halo, such as chloro or fluoro

(e) aromatic heterocycle of 5 or 6 members selected from furyl, pyridyl, and thienyl either unsubstituted or substituted with R.sup.17 R.sup.18 N--C.sub.1-3 alkyl

(f) --NR.sup.17 R.sup.18, and

(g) C.sub.2-5 alkyl substituted with --NR.sup.17 R.sup.18 ;

R.sup.16 is

(a) hydrogen, or

(b) C.sub.1-3 alkyl;

with the proviso that if R.sup.14 is hydrogen, one of R.sup.15 and R.sup.16 is other than hydrogen, which comprises treating a compound of structural formula: ##STR29## with dimethyldichlorosilane and sodium iodide in an acetonitrile at about 75.degree. to 100.degree. C. for about one to 4 hours.

2. The process of claim 1 for preparing the compound of formula ##STR30##
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