- Visible Light-Induced Amide Bond Formation
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A metal-, base-, and additive-free amide bond formation reaction was developed under an organic photoredox catalyst. This green approach showed excellent functional selectivity without affecting other functional groups such as alcohols, phenols, ethers, esters, halogens, or heterocycles. This method featured a broad substrate scope, good compatibility with water and air, and high yields (≤95%). The potential utilities were demonstrated by the synthesis of important drug molecules such as paracetamol, melatonin, moclobemide, and acetazolamide.
- Song, Wangze,Dong, Kun,Li, Ming
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supporting information
p. 371 - 375
(2019/11/29)
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- Preparation process for intermediate of acetazolamide
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The invention especially relates to a preparation process for an intermediate of acetazolamide, belonging to the field of medicine synthesis. The process comprises the following steps: with thiosemicarbazide and carbon disulfide as reactants and a mixture of pyridine and piperidine as a solvent, carrying out a reaction; and then successively carrying out purification and drying so as to obtain 2-amino-5-mercapto-1,3,4-thiadiazole, i.e., the intermediate of acetazolamide.
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Paragraph 0052; 0053
(2017/09/13)
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- Compositions and methods for the suppression of carbonic anhydrase activity
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The invention relates to the compounds of formula I or its pharmaceutical acceptable salts, as well as polymorphs, solvates, enantiomers, stereoisomers and hydrates thereof. The pharmaceutical compositions comprising an effective amount of compounds of formula I, and methods for treating or preventing or modulating carbonic anhydrase activity in a disease may be formulated for oral, buccal, rectal, topical, transdermal, transmucosal, intravenous, parenteral administration, syrup, or injection. Such compositions may be used to treatment of glaucoma, epileptic seizures, Idiopathic intracranial hypertension (pseudotumor cerebri), altitude sickness, cystinuria, periodic paralysis and dural ectasia, congestive heart failure, drug induced edema, diuretic, intermittent claudication resulting from obstructed arteries in the limbs, and vascular dementia.
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Page/Page column 27; 28
(2016/04/05)
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- Key intermediate aqiang 2-acetyl-5-chlorosulfonyl -1, 3, 4-thiadiazole method for preparing the non-chlorine (by machine translation)
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The invention discloses a preparation method of non-chlorine gas of acetazolamide key intermediate 2-acetamido-5-chlorosulfonyl-1, 3, 4-thiadiazole. The preparation method comprises the steps of firstly adding hydrochloric acid into a reactor and then dropwise adding hydrogen peroxide to perform reaction so as to obtain a reaction solution; adding 2-acetamido-5-sulfydryl-1, 3, 4-thiadiazole into the obtained reaction solution in batch to perform reaction and obtaining a reactant after reaction is completed; directly conducting suction filtration, washing and drying on the reactant and performing drying to obtain the intermediate 2-acetamido-5-chlorosulfonyl-1, 3, 4-thiadiazole. The preparation method is more moderate in operate and more environment-friendly, and the obtained intermediate 2-acetamido-5-chlorosulfonyl-1, 3, 4-thiadiazole is good in color and luster and high in purity.
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Paragraph 0037
(2017/01/02)
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- COMPOSITIONS AND METHODS FOR SUPPRESSION OF CARBONIC ANHYDRASE ACTIVITY
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Provided are the compounds of formula (I) or its pharmaceutical acceptable salts, as well as polymorphs, solvates, enantiomers, stereoisomers and hydrates thereof. The pharmaceutical compositions comprising an effective amount of compounds of formula (I), and methods for treating or preventing or modulating carbonic anhydrase activity in a disease may be formulated for oral, buccal, rectal, topical, transdermal, transmucosal, intravenous, parenteral admimstration, syrup, or injection. Such compositions may be used to treatment of glaucoma, epileptic seizures, Idiopathic intracranial hypertension (pseudotumor cerebri), altitude sickness, cystinuria, periodic paralysis and dural ectasia, congestive heart failure, drug induced edema, diuretic, intermittent claudication resulting from obstructed arteries in the limbs, and vascular dementia.
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Paragraph 0098; 0099
(2013/12/03)
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- Preparation of sulfonamides from N-silylamines
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Sulfonamides have been prepared in high yields by the reactions of N-silylamines with sulfonyl chlorides and fluorides. In a competition experiment, the sulfonyl chlorides were found to be far more reactive than sulfonyl fluorides. The chemistry may be used to prepare aliphatic, aromatic, tertiary, secondary, and primary sulfonamides. It may also be done in the absence of solvent and the byproduct trimethylsilyl chloride recovered in good yield. Primary sulfonamides were synthesized from the sulfonyl chloride with aminotriphenyl silane (Ph3SiNH2), a conversion demonstrated with the synthesis of the carbonic anhydrase inhibitor, acetazolamide.
- Naredla, Rajasekhar Reddy,Klumpp, Douglas A.
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supporting information
p. 5945 - 5947
(2013/10/22)
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- Synthesis and hydrolysis kinetic study of few co-drugs of propranolol and other antihypertensive drugs
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The different acyl halide analogs of propranolol were synthesized by reacting Propanolol with different acyl anhydrides in toluene medium. The derivatives were reacted with thionyl chloride to get propranolol hemi acyl chloride. Finally the co-drugs were synthesized by reacting propranolol hemi acyl chloride with different classes of antihypertensive drugs like Nifedepine (PSN,PMN,PPN), Hydrochlorthiazide (PSH, PMH, PPH) and Acetazolamide(PSA, PMA, PPA) by ester linkage. The structure of the synthesized derivative of propranolol analogs were confirmed by M P, TLC, IR and NMR data.
- Baidya, Mayukh,Das, Amit Kumar
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body text
p. 173 - 178
(2012/01/13)
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- GIAO/DFT 13C NMR Chemical Shifts of 1,3,4-thiadiazoles
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1H, 13C and 15N NMR spectra of 2-acetylamino-1,3,4-thiadiazole and its 5-substituted derivatives have been measured and assigned based on reference data, as well as homo- and heteronuclear 2 D NMR experiments. In addition, the GIAO/DFT approach at the B3LYP level of theory using the 6-311G basis set was used to calculate the 13C NMR chemical shifts. Although this method gives reliable results for 2-arylhydrazones of 1,3-diphenylpropanetrione, 2-phenacylpyridines, (Z)-2-(2-hydroxy-2-phenylvinyl)pyridines, 4-fluoroanilines, (1Z,3Z)-1,4-di(pyridin-2-yl)buta-1,3-dienediols and their tautomeric forms, the calculated chemical shifts for the 1,3,4-thiadiazoles studied are less satisfactory. Presence of the sulfur atom(s) seems to be responsible for such behavior.
- Loghmani-Khouzani, Hossein,Rauckyte, Teresa,Osmialowski, Borys,Gawinecki, Ryszard,Kolehmainen, Erkki
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p. 2217 - 2225
(2008/02/10)
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- Process and device for producing liquid dosage formulations of medicinal compounds on demand from tablets and capsules
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The present invention provides a process for preparing liquid pharmaceutical formulations on demand from tablets and capsules.
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- Synthesis of certain diarylsulfonylureas as antitumor agents
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A new series of N-aryl-N′-heteroaryl or N,N′-diheteroaryl sulfonylurea or sulfonylthiourea was synthesized and screened for their antitumor activity at the National Cancer Institute (NCI). N-(3-Chlorophenyl)-N′-(6-methyl-uracil-2-sulfonyl)urea (28) with GI50, TGI, LC50 (MG-MID) values of 66.1, 83.2, 93.3 μM, respectively is the most active compound in this study. It showed a remarkable activity more than sulofenur against HL-60 (TB) and RPMI-8226 leukemia, HOP-92 Non small lung cancer, KM12 colon cancer, SF-295 CNS cancer, PC-3 prostate cancer, OVCAR-4 Ovarian cancer, CAKI-1 and UO-31 Renal cancer, and MDA-MB-435 Breast cancer with GI50 values of 0.3, 2.7, 6.9, 14.7, 8.2, 9.3, 2.0, 2.1, 3.4, 11.3 μM, respectively.
- Youssef,Al-Abdullah,El-Khamees
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p. 404 - 418
(2007/10/03)
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- Synthesis and investigation of inhibition effects of new carbonic anhydrase inhibitors
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Three new derivatives of 2-substituted 1,3,4-thiadiazole-5-sulfonamide have been synthesized. These compounds are 2-(3-chloropropionylamino)- 1,3,4-thiadiazole-5-sulfonamide (1); 2-(2,2-dichloroacetylamino)-1,3,4-thiadiazole-5-sulfonamide (2); and 2-(3-phenylpropionylamino)-1,3,4-thiadiazole-5-sulfonamide (3). Inhibition effects of these compounds on carbonic anhydrase I and II have been investigated. By comparing 150 and K(i) values of the compounds, it has been found that compound 1 is a more potent inhibitor than acetazolamide (b) on carbonic anhydrase II.
- Arslan, Oktay,Kuefrevioglu, Oe. Irfan,Nalbantoglu, Barbaros
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p. 515 - 518
(2007/10/03)
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- Combination of two active substances
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The invention concerns the use of a compound with diuretic properties and of a magnesium supplementation in the form of magnesium monoaspartate hydrochloride, magnesium oxide, magnesium hydroxide or magnesium carbonate, and optionally of a potassium supplementation, and pharmaceutical preparations comprising a compound with diuretic properties and a magnesium supplementation in the form of magnesium monoasparate hydrochloride, magnesium oxide, magnesium hydroxide, or magnesium carbonate and optionally a potassium supplementation.
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- Gastric cytoprotection with heterocyclic sulfonamides
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The present invention provides a method for gastrointestinal cytoprotection using a class of heterocyclic sulfonamides.
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