41457-31-2

Upstream product

• 5790-06-7 1-Chloro-3-(2,3-dimethyl-phenoxy)-propan-2-ol 
• 526-75-0 2,3-Dimethylphenol 
• 3132-64-7 1,2-Epoxy-3-bromopropane 
• 106-89-8 epichlorohydrin 

Downstream Products

• 91623-00-6 5-<3-(2,3-dimethylphenoxy)-2-hydroxypropyl>-6a,7,8,9-tetrahydropyrido<3,2-e>pyrrolo<1,2-a>pyrazin-6(5H)-one 
• 91623-00-6 5-<3-(2,3-dimethylphenoxy)-2-hydroxypropyl>-6a,7,8,9-tetrahydropyrido<3,2-e>pyrrolo<1,2-a>pyrazin-6(5H)-one 
• 111794-54-8 3-{Benzyl-[3-(2,3-dimethyl-phenoxy)-2-hydroxy-propyl]-amino}-N-[4-(4-methyl-6-oxo-1,4,5,6-tetrahydro-pyridazin-3-yl)-phenyl]-propionamide 
• 64980-33-2 1-(2,3-Dimethylphenoxy)propan-2-ol 
• 64980-39-8 1-Isopropylthio-3-(2,3-dimethylphenoxy)propan-2-ol 
• 30187-90-7 1-(2,3-dimethylphenoxy)-3-((1,1-dimethylethyl)amino)-2-propanol 
• 111794-27-5 3-[3-(2,3-Dimethyl-phenoxy)-2-hydroxy-propylamino]-N-[4-(4-methyl-6-oxo-1,4,5,6-tetrahydro-pyridazin-3-yl)-phenyl]-propionamide 
• 100822-58-0 4-(2,3-Dichlorophenyl)-7-[3-(2,3-dimethylphenoxy)-2-hydroxypropyl]-1,4,5,6,7,8-hexahydro-2-methyl-5-oxo-1,7-naphthyridine-3-carboxylic acid methyl ester 
• 256372-73-3 (S)-1-(2',3'-dimethylphenoxy)-2,3-epoxypropane 
• 64980-36-5 1-Isopropylamino-4-(2,3-dimethylphenoxy)butan-3-ol 
• 802287-59-8 1-(2,3-dimethyl-phenoxy)-3-methylamino-propan-2-ol 
• 64980-38-7 1-Isopropyloxy-3-(2,3-dimethylphenoxy)propan-2-ol 

Relevant academic research and scientific papers

NBS/DMSO-mediated synthesis of (2,3-dihydrobenzo[b] [1,4]oxathiin-3-yl)methanols from aryloxymethylthiiranes

(2,3-Dihydrobenzo[b][1,4]oxathiin-3-yl)methanols were synthesized via reactions of aryloxymethylthiiranes and N-bromosuccinimide (NBS) in DMSO under microwave irradiation. The reaction mechanism was proposed as an intramolecular aromatic electrophilic substitution of 1-bromo-2-(aryloxymethyl)thiiran-1-iums, generated from aryloxymethylthiiranes and NBS, and the subsequent DMSO nucleophilic ring opening reaction of thiiran-1-iums followed by the water displacement. The current method provides a direct and simple strategy in the efficient preparation of (2,3-dihydrobenzo[b][1,4]oxathiin-3-yl)methanols from readily available aryloxymethylthiiranes.

A smart library of epoxide hydrolase variants and the top hits for synthesis of (S)-β-blocker precursors

Microtuning of the enzyme active pocket has led to a smart library of epoxide hydrolase variants with an expanded substrate spectrum covering a series of typical β-blocker precursors. Improved activities of 6- to 430-fold were achieved by redesigning the active site at two predicted hot spots. This study represents a breakthrough in protein engineering of epoxide hydrolases and resulted in enhanced activity toward bulky substrates. Hot pockets: Microtuning of the enzyme active pocket gives a smart library of epoxide hydrolase variants with an expanded substrate spectrum covering a series of typical β-blocker precursors. Improved activities of 6- to 430-fold were achieved by redesigning the active site at two predicted hot spots, and enhanced activity toward bulky substrates was found.

CATHEPSIN PROTEASES INHIBITORS

The invention provides compounds (I) and pharmaceutical compositions thereof, and more particularly, bicyclic carbamates, which are useful as cathepsin inhibitors, and methods for using such compounds or pharmaceutically acceptable salts thereof, wherein

Bicyclic carbamates as inhibitors of papain-like cathepsin proteases

A 6-oxa-1-aza-bicyclo[3.2.1]octan-7-one system inhibits the proteolytic activity of several cysteine proteases belonging to the papain family. In vitro mechanistic studies and in silico calculations suggest that the minimal π-overlap between the bridgehea

Design and synthesis of a series of combined vasodilator/β-adrenoceptor antagonists based on 6-arylpyridazinones

A series of new 6-[4-[[(aryloxy)acyl]amino]phenyl]-4,5-dihydropyridazinones have been synthesized and evaluated as combined vasodilator/β-adrenoceptor antagonists and potential antihypertensive agents. Many of the early compounds displayed an unacceptably high level of intrinsic sympathomimetic activity (ISA) and a relatively short duration of action. Disubstitution in the 2,3-positions or in the 4-position of the aryloxy ring gave compounds with low ISA levels and, in some instances, improved duration of action. All of the compounds were vasodilators, but the 5-methylpyridazinone derivatives showed consistently greater antihypertensive activity than their 5-H lower homologues. Further detailed pharmacological investigations led to the selection of 6-[4-[3-[[2-hydroxy-3-[4-[2-(cyclopropylmethoxy)ethyl]phenoxy]propyl]amino ]propionamido]phenyl]-5-methyl-4,5-dihydro-3(2H)-pyridazinone (4t) (SK&F 95018) as a development candidate.

Antihypertensive indole derivatives of phenoxypropanolamines with β-adrenergic receptor antagonist and vasodilating activity

A series of 25 aryloxypropanolamines containing the 3-indolyl-tert-butyl[i.e., 1,1-dimethyl-2-(1H-indol-3-yl)ethyl] or substituted 3-indolyl-tert-butyl moiety as the N substituent is reported. These compounds have been tested for antihypertensive activity in spontaneously hypertensive rats (SHR), β-adrenergic receptor antagonist action in conscious normotensive rats, vasodilating activity in ganglion-blocked rats with blood pressure maintained by angiotensin II infusion, and for intrinsic sympathomimetic action (ISA) in reserpinized rats. Some of the compounds exhibit antihypertensive activity in combination with β-adrenergic receptor antagonist and vasodilating action. The structure-activity relationships in these tests are discussed.