42908-86-1

Usage

Synthesis Reference(s)

Tetrahedron Letters, 14, p. 5121, 1973 DOI: 10.1016/S0040-4039(01)87403-7

Upstream product

• 87-41-2 2-benzofuran-1(3H)-one 
• 88-95-9 Phthaloyl dichloride 
• 933-88-0 ortho-toluoyl chloride 
• 2526-64-9 dichlorotriphenylphosphorane 
• 7782-50-5 chlorine 
• 118-90-1 ortho-methylbenzoic acid 
• 612-20-4 2-(hydroxymethyl)benzoic acid 

Downstream Products

• 109047-46-3 2-chloro-1-(2-chloromethyl-phenyl)-ethanone 
• 1531-78-8 o-(chloromethyl)benzoic acid ethyl ester 
• 85888-81-9 2-(chloromethyl)benzoic acid 
• 57723-12-3 4-phenyl-3-(2-pyrrolidin-1-yl-ethylimino)-3,4-dihydro-1H-benzo[e][1,3]thiazepin-5-one 
• 57723-13-4 4-phenyl-2-(2-pyrrolidin-1-yl-ethyl)-3-thioxo-2,3,4,5-tetrahydro-benzo[e][1,3]diazepin-1-one 
• 58531-18-3 3-allylimino-4-phenyl-3,4-dihydro-1H-benzo[e][1,3]thiazepin-5-one 
• 57723-21-4 4-allyl-3-phenylimino-3,4-dihydro-1H-benzo[e][1,3]thiazepin-5-one 
• 57723-22-5 2-allyl-4-phenyl-3-thioxo-2,3,4,5-tetrahydro-benzo[e][1,3]diazepin-1-one 
• 57723-14-5 3-(2-morpholin-4-yl-ethylimino)-4-phenyl-3,4-dihydro-1H-benzo[e][1,3]thiazepin-5-one 
• 57722-86-8 4-o-tolyl-3-o-tolylimino-3,4-dihydro-1H-benzo[e][1,3]thiazepin-5-one 
• 57722-93-7 2,4-bis-(4-methoxy-benzyl)-3-thioxo-2,3,4,5-tetrahydro-benzo[e][1,3]diazepin-1-one 
• 57722-89-1 4-(4-methyl-benzyl)-3-(4-methyl-benzylimino)-3,4-dihydro-1H-benzo[e][1,3]thiazepin-5-one 
• 57723-15-6 3-(3-dimethylamino-propylimino)-4-phenyl-3,4-dihydro-1H-benzo[e][1,3]thiazepin-5-one 
• 57723-11-2 3-(2-diethylamino-ethylimino)-4-phenyl-3,4-dihydro-1H-benzo[e][1,3]thiazepin-5-one 

Relevant academic research and scientific papers

Kresoxim-methyl Derivatives: Synthesis and Herbicidal Activities of (Pyridinylphenoxymethylene)phenyl Methoxyiminoacetates

A series of new kresoxim-methyl derivatives, (pyridinylphenoxymethylene)phenyl methoxyiminoacetates, were synthesized and their structures were confirmed by NMR and high-resolution mass spectrometry (HRMS). Although derived from a fungicide, the bioassays indicated that several new compounds had good herbicidal activities. At 37.5 g a.i./ha, compound 5c showed 100% inhibition against Abutilon theophrasti, Amaranthus retroflexus, and Eclipta prostrata, which was better than mesotrione. Compound 5e had a broad herbicidal spectrum against broadleaf weeds. The present work indicates that 5c and 5e may serve as new candidates for potential herbicides.

Polyfluoroalkyl-containing isoindolinone benzamide derivative, preparation method and application thereof

The invention provides a polyfluoroalkyl-containing isoindolinone benzamide derivative, which has the following general formula A-1 as shown in the specification, wherein substituent groups are shown as the specification. The polyfluoroalkyl-containing isoindolinone benzamide derivative provided by the invention is suitable for agricultural insecticide.

The synthesis of 3-cyano-2-(organylamino)thieno[3,2-c]isoquinoline derivatives

A method for the preparation of 3-cyano-2-(organylamino)thieno[3,2-c]isoquinoline derivatives has been developed. Alkylation of (2,2-dicyano-1-organylaminovinyl)thiolates with methyl 2-(chloromethyl)benzoate or N-substituted 2-(chloromethyl)benzamides with the subsequent treatment of the alkylation products with potassium tert-butoxide gave 3-cyano-2-(organylamino)thieno[3,2-c]isoquinolin-5(4H)-ones. In the case of utilization of (chloromethyl)benzonitrile in this synthesis, 5-amino-3-cyano-2-organylaminothieno[3,2-c]iso-quinolines were obtained.

Synthesis of 5-aminopyrido[3′,2′:4,5]thieno[3,2-c]isoquinoline derivatives from 3-cyanopyridine-2(1H)-thiones and 2-(chloromethyl)benzamide

Substituted 5-aminopyrido[3′,2′:4,5]thieno[3,2-c]isoquinolines were synthesized by condensation of substituted 3-cyanopyridine-2(1H)-thiones with 2-(chloromethyl)benzamide and subsequent treatment of the condensation products with potassium tert-butoxide. Oxidation of the condensation products to sulfoxides and sulfones followed by treatment of these compounds with potassium tert-butoxide gives substituted 5-aminopyrido[3′,2′:4,5]thieno[3,2-c]isoquinoline 11-oxides and substituted 5-aminopyrido[3′,2′:4,5]thieno[3,2-c]isoquinoline 11,11-dioxides in good yields.

SGC STIMULATORS

Compounds of Formula (I) are described. They are useful as stimulators of sGC, particularly NO-independent, heme-dependent stimulators. These compounds may be useful for treating, preventing or managing various disorders that are herein disclosed.

Crucial role of selenium in the virucidal activity of benzisoselenazol- 3(2h)-ones and related diselenides

Various N-substituted benzisoselenazol-3(2H)-ones and their non-seleniumcontaining analogues have been synthesized and tested against selected viruses (HHV-1, EMCV and VSV) to determine the extent to which selenium plays a role in antiviral activity. The data presented here show that the presence of selenium is crucial for the antiviral properties of benzisoselenazol-3(2H)-ones since their isostructural analogues having different groups but lacking selenium either did not show any antiviral activity or their activity was substantially lower. The open-chain analogues of benzisoselenazol- 3(2H)-ones-diselenides also exhibited high antiviral activity while selenides and disulfides were completely inactive towards model viruses.

TERTIARY ALKYL ESTER OF OXODIBENZOXEPIN ACETIC ACID

A tertiary alkyl ester represented by Formula (2): wherein R1 and R2 each independently represent a C1-4 alkyl group, and a method for producing the same.

EFFICIENT ASPIRIN PRODRUGS

Aspirin is one of the most widely used drugs in the treatment of inflammation, pain and fever. It has more recently found application in the prevention of heart attacks and stroke and is being studied as a cancer chemopreventative agent. Despite its value aspirin continues to be underutilized because it causes gastric bleeding. The technology under development potentially removes this problem. It is designed to reduce contact between the drug and the intestinal lining. An isosorbide aspirinate prodrug compound is thus provided. The compound has the general structure as shown in general formula (I) wherein Y is a C1 - C8 alkyl ester, a C1 - C8 alkoxy ester, a C3 - C10 cycloalkyl ester, an arylester, a C1 - C8 alkylaryl ester or -C(O)ORring, wherein Rring is a 5-membered aromatic or nonaromatic 5-member ring having at least one heteroatom substituted for a carbon of the ring system, which can be unsubstituted or substituted with at least one nitric oxide releasing group.

Isosorbide-based aspirin prodrugs: Integration of nitric oxide releasing groups

Aspirin prodrugs and related nitric oxide releasing compounds hold significant therapeutic promise, but they are hard to design because aspirin esterification renders its acetate group very susceptible to plasma esterasemediated hydrolysis. Isosorbide-2-aspirinate-5-salicylate is a true aspirin prodrug in human blood because it can be effectively hydrolyzed to aspirin upon interactionwith plasma BuChE. We show that the identity of the remote 5-ester dictates whether aspirin is among the products of plasma-mediated hydrolysis. By observing the requirements for aspirin release from an initial panel of isosorbide-based esters,we were able to introduce nitroxymethyl groups at the 5-position while maintaining ability to release aspirin. Several of these compounds are potent inhibitors of platelet aggregation. The design of these compounds will allow better exploration of cross-talk between COX inhibition and nitric oxide release and potentially lead to the development of selective COX-1 acetylating drugs without gastric toxicity.

Nitroderivatives as drugs for diseases having an inflammatory basis

Use for the treatment of diseases having an inflammatory basis of compounds or salts thereof, having the following general formula (I): A-Xt-L-(W)p—NO2 wherein A contains the radical of a drug, Xt and W arc bivalent radicals, L, is a covalent bond or oxygen, sulphur, NRtc wherein Rtc is H or a C1-C5 linear or branched alkyl.