Generated: May 22, 2017
|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|
|Claims:||1. A process for preparing a compound of structural formula: ##STR30## wherein R.sup.13 is |
(b) phenyl either unsubstituted or substituted with one or more of
(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,
(d) .dbd.O; or
(e) --NR.sup.17 R.sup.18
(c) phenyl-C.sub.1-3 alkyl, wherein the phenyl is either unsubstituted or substituted with one or more of
(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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