130693-82-2 Usage
Description
Different sources of media describe the Description of 130693-82-2 differently. You can refer to the following data:
1. Dorzolamide hydrochloride was introduced in the U.S.A. as eye drops
for the treatment of open-angle glaucoma and ocular hypertension. Dorzolamide is a
potent carbonic anhydrase inhibitor that, on topical administration, lowers intraocular
pressure (IOP). In a clinical study in patients with bilateral primary open-angle
glaucoma or ocular hypertension, dorzolamide (0.7-2%) was found to significantly lower
IOP throughout the day. Dorzolamide has been shown to be effective as a single
therapy or in combination with β-blockers.
2. Dorzolamide (hydrochloride) (Item No. 26303) is an analytical reference standard categorized as a carbonic anhydrase inhibitor diuretic. Diuretics have been used in sports doping to reduce weight or anabolic androgenic steroid-induced water retention, or as masking agents. This product is intended for use in analytical forensic applications. This product is also available as a general research tool .
Chemical Properties
White Powder
Originator
Merck (U.S.A.)
Uses
Different sources of media describe the Uses of 130693-82-2 differently. You can refer to the following data:
1. Carbonic anhydrase inhibitor. Antiglaucoma agent.
2. Antiglaucoma drug;Carbonic anhydrase inhibitor
3. analgesic
4. Dorzolamide HCl Ophthalmic Solution is indicated in the treatment of elevated intraocular pressure in patients with ocular hypertension or open-angle glaucoma.
5. An inhibitor of carbonic anhydrase.
Definition
ChEBI: The hydrochloride salt of dorzolamide. It is used in ophthalmic solutions to lower increased intraocular pressure in the treatment of open-angle glaucoma and ocular hypertension.
Manufacturing Process
Manufacturing process for Dorzolamide hydrochloride includes these steps as follows: Step A: Sulfuric Acid Ritter Procedure;Step B: Sulfonylation Procedure Step C: Chlorosulfonylation Procedure;Step D: Amidation Procedure;Step E: Reduction via Borane Generated in situ Procedure;Step F: Maleate Salt Formation Procedure;Step G: Crude Hydrochloride Salt Formation;Step H: Recrystallization Procedure.
Therapeutic Function
Antiglaucoma
Veterinary Drugs and Treatments
Dorzolamide is often used in the contralateral eye of a dog with
primary glaucoma to prevent development of bilateral disease. It
is also an excellent agent to consider for most secondary glaucomas
in dogs and cats because it has no effect on pupil size. Like the
related oral carbonic anhydrase inhibitors (dichlorphenamide or
Daranide?, methazolamide or Neptazane?), dorzolamide decreases
aqueous humor production by the ciliary body epithelium by altering
pH and affecting the H+/Na+ active transport exchange mechanism.
Oral carbonic anhydrase inhibitors cause numerous systemic
side effects such as metabolic acidosis and panting, diarrhea, vomiting,
anorexia and others, all of which can be avoided with topical
carbonic anhydrase inhibitors.
Check Digit Verification of cas no
The CAS Registry Mumber 130693-82-2 includes 9 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 6 digits, 1,3,0,6,9 and 3 respectively; the second part has 2 digits, 8 and 2 respectively.
Calculate Digit Verification of CAS Registry Number 130693-82:
(8*1)+(7*3)+(6*0)+(5*6)+(4*9)+(3*3)+(2*8)+(1*2)=122
122 % 10 = 2
So 130693-82-2 is a valid CAS Registry Number.
InChI:InChI=1/C10H16N2O4S3.ClH/c1-3-12-8-4-6(2)18(13,14)10-7(8)5-9(17-10)19(11,15)16;/h5-6,8,12H,3-4H2,1-2H3,(H2,11,15,16);1H/t6-,8-;/m0./s1
130693-82-2Relevant articles and documents
Chiral synthesis method of dorzolamide hydrochloride
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Paragraph 0023-0027, (2021/09/04)
The invention relates to a chiral synthesis method of dorzolamide hydrochloride, which comprises the following steps: (1) by taking a compound I that is (6S)-4-carbonyl-5,6-dihydro-4H-6-methyl-thieno[2,3b] thiopyran-2-sulfonamide-7,7-dioxide as an initial raw material, carrying out imidization reaction on the initial raw material and ethylamine to obtain a compound II that is (6S)-4-ethyl imino-5,6-dihydro-4H-6-methyl-thieno[2, 3b]thiopyran-2-sulfonamide-7,7-dioxide; (2) carrying out asymmetric hydrogenation reaction on the compound II obtained in the step (1), a catalyst and a chiral ligand (R)-(+)-1,1'-binaphthyl-2'-isopropoxy-2-diphenylphosphine to obtain a compound III that is dorzolamide; and (3) mixing the compound III obtained in the step (2) with hydrochloric acid, acidifying, washing and drying to obtain a compound IV, namely dorzolamide hydrochloride. The synthesis method is simple and easy to implement, high in chiral selectivity and low in cost, and the obtained dorzolamide hydrochloride is high in purity and suitable for industrial production.
PROCESS FOR THE PREPARATION OF DORAOLZMIDE HYDROCHLORIDE
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Page/Page column 13, (2018/04/21)
The present invention discloses an improved process for the preparation of dorzolamide hydrochloride the compound of Formula I.
PROCESS FOR PREPARING ENANTIOMERICALLY ENRICHED OXAMIDES
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Page/Page column 15; 16, (2014/01/18)
The present invention relates to a chiral oxamide of formula (I) useful as an intermediate in the preparation of dorzolamide, and to the preparation thereof. The invention also relates to the preparation of dorzolamide, to the hydrochloride salt thereof, and to the active ingredient contained in a drug useful in the treatment of glaucoma, by means of the intermediate of formula (I).