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Generated: December 16, 2017

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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), Habecker; Charles N. (Lansdale, PA)
Assignee: Merck & Co., Inc. (Rahway, NJ)
Filing Date:Apr 04, 1988
Application Number:07/177,211
Claims:1. A process for preparing a compound of structural formula: ##STR30## wherein R.sup.13 is

(a) hydrogen,

(b) 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.1-5 alkyl, wherein R.sup.17 and R.sup.18 are independently selected from:

(i) hydrogen or

(ii) C.sub.1-5 alkyl, or taken together with the nitrogen to which they are attached from a heterocycle selected from morpholine, piperidine, pyrrolidine, and piperazine,

(c) --OH,

(d) .dbd.O; or

(e) --NR.sup.17 R.sup.18

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,

which comprises treating a compound of structural formula: ##STR31## with Oxone.RTM. (potassium peroxymonosulfate) in an aqueous ethanolic solution to provide the compound of formula: ##STR32## followed by treatment with an amine of formula R.sup.17 R.sup.18 NH in a C.sub.1-3 alkanol at 12.degree.-30.degree. C. for 5 to 24 hours.

2. The process of claim 1, wherein R.sup.13 and R.sup.14 are both hydrogen.

3. The process of claim 2, wherein 5,6-dihydro-6-methylene-4H-thieno[2,3-b]thiopyrano-2-sulfonamide-7,7-dioxi de is treated with isobutylamine to form ##STR33##
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