5819-19-2

Usage

InChI:InChI=1/C9H9ClO2/c1-7(10)12-9(11)8-5-3-2-4-6-8/h2-7H,1H3

Upstream product

• 769-78-8 vinyl benzoate 
• 98-88-4 benzoyl chloride 
• 75-07-0 acetaldehyde 
• 7647-01-0 hydrogenchloride 
• 123-63-7 paracetaldehyde 

Downstream Products

• 132750-16-4 Benzoic acid 1-[2-(pyridin-2-ylmethylsulfanyl)-benzoimidazol-1-yl]-ethyl ester 
• 103312-98-7 2-<(2-pyridinylmethyl)sulfinyl>-1H-benzimidazole-1-ethan-2-ol benzoate 
• 141872-48-2 1-(Benzoyloxy)ethyl 4-{N-butyl-N-[(2'-[N-triphenylmethyl-1H-tetrazol-5-yl]biphenyl-4-yl)methyl]amino}pyrimidine-5-carboxylate 
• 141871-99-0 1-(Benzoyloxy)ethyl 4-{N-butyl-N-[(2'-[1H-tetrazol-5-yl]biphenyl-4-yl)methyl]amino}pyrimidine-5-carboxylate 
• 769-78-8 vinyl benzoate 
• 1391034-27-7 C₁₂H₁₄O₃S₂ 
• 666174-90-9 (S)-1-chloroethyl benzoate 
• 666174-89-6 (R)-benzoic acid 1-chloroethyl ester 
• 581106-33-4 [3-[acetyl(phenylmethoxy)amino]propyl]-phosphonic acid bis[1-(benzoyloxy)ethyl] ester 
• 52571-16-1 1-iodoethyl benzoate 

Relevant academic research and scientific papers

Method for synthesizing vinyl carboxylate

The present invention relates to a method for synthesizing carboxylic acid enol esters, in particular to a method for synthesizing vinyl carboxylate. The vinyl carboxylate is prepared by performing asynergistic reaction on a 1-chloroethyl carboxylate represented by a formula 1 and an epoxy compound under the effect of a metal chloride catalyst. In 1-chloroethyl carboxylate represented by the formula 1, n is a natural number larger than or equal to 1, when n=1, the 1-chloroethyl carboxylate includes monocarboxylates in which R represents a hydrocarbon group or a hetero-hydrocarbon group containing carbonyl, an ether bond, a thioether bond, an ester bond, or a peptide bond, and when n is equal to or larger than 2, the 1-chloroethyl carboxylate ester includes di(1-chloroethyl) oxalate and polycarboxylates in which R is a hydrocarbon group or a hetero-hydrocarbon group containing carbonyl, an ether bond, a thioether bond, an ester bond and a peptide bond. Compared with a vinyl acetate exchange method, the synergic method has a lower cost, and the process design is simple and suitable for industrial production. The vinyl carboxylate has a wide range of uses in the field of polymer synthesis and coatings.

NO-RELEASING NONOATE (NITROGEN-BOUND) SULFONAMIDE-LINKED-COXIB ANTI-CANCER AGENTS

The present invention provides NO-releasing NONOate(nitrogen bound)sulfonamide- linked-coxib anti-cancer agents, having the structure of Formula (I): wherein R1, X, L, R2, R3, R4, and Z are as defined in the detailed description; pharmaceutical compositions comprising at least one compound of Formula (I); and methods useful for healing wounds, preventing and treating cancer, or treating actinic keratosis, cystic fibrosis or acne, using a compound of Formula (I).

COMPOUNDS AND THERAPEUTIC USES THEREOF

The invention relates to compounds, pharmaceutical compositions and methods useful for treating cancer, systemic or chronic inflammation, rheumatoid arthritis, diabetes, obesity, T-cell mediated autoimmune disease, ischemia, and other complications associated with these diseases and disorders.

A short formal total synthesis of (±)-hirsutic acid

A short formal total synthesis of (±)-hirsutic acid is described using a Claisen rearrangement and a radical cascade as the key steps. The radical sequence involves an intermolecular addition of a radical derived from a xanthate followed by a cyclization and transfer of the xanthate group.

Prodrugs of perzinfotel with improved oral bioavailability

Previous studies with perzinfotel (1), a potent, selective, competitive NMDA receptor antagonist, showed it to be efficacious in inflammatory and neuropathic pain models. To increase the low oral bioavailability of 1 (3-5%), prodrug derivatives (3a-h) were synthesized and evaluated. The oxymethylene-spaced diphenyl analogue 3a demonstrated good stability at acidic and neutral pH, as well as in simulated gastric fluid. In rat plasma, 3a was rapidly converted to 1 via 2a. Pharmacokinetic studies indicated that the amount of systemic exposure of 1 produced by a 10 mg/kg oral dose of 3a was 2.5-fold greater than that produced by a 30 mg/kg oral dose of 1. Consistent with these results, 3a was significantly more potent and had a longer duration of activity than 1 following oral administration in a rodent model of inflammatory pain. Taken together, these results demonstrate that an oxymethylene-spaced prodrug approach increased the bioavailability of 1.

DERIVATIVES OF 2-(8,9-DIOXO-2,6-DIAZABICYCLO(5.2.0)NON-1(7)-EN-2-YL)ALKYL PHOSPHONIC ACID AND THEIR USE AS N-METHYL-D-ASPARTATE (NMDA) RECETOR ANTAGONISTS

Compounds of formula (I) or pharmaceutically acceptable salts thereof are provided where at least one of R2 or R3 is not hydrogen. The compounds of the present invention are N-methyl-D-aspartate (NMDA) receptor antagonists and are useful in treating a variety of conditions present in a mammal that benefit from inhibiting the NMDA receptor.

BETA-LACTAMASE INHIBITOR PRODRUG

Prodrugs of 6-?-hydroxymethylpenicillanic acid sulfone having the structure wherein R is H or methyl, and solvates thereof, are disclosed. Also disclosed are pharmaceutical compositions comprising a prodrug of the present invention, or a solvate thereof, an optional beta-lactam antibiotic and at least one pharmaceutically acceptable carrier. Further disclosed is a method for increasing the therapeutic effectiveness of a beta-lactam antibiotic in a mammal by administering an effective amount of a betalactam antibiotic and an effectiveness-increasing amount of a prodrug of the present invention, or a solvate thereof. Additionally disclosed is a method for treating a bacterial infection in a mammal by administering a therapeutically effective amount of a pharmaceutical composition of the present invention to a mammal in need thereof.

Prodrugs of CL316243: A selective β3-adrenergic receptor agonist for treating obesity and diabetes

CL316243 is a highly selective and potent β3-adrenergic receptor agonist, and has been shown in rodent models to be an effective agent for treating obesity and Type II diabetes. To improve the oral absorption and pharmacokinetic profiles of CL316243, a number of prodrugs have been synthesized and evaluated. Several ester-type prodrugs show significant improvements in oral bioavailability in both rodent and primate models.

Anti-inflammatory 2-methyl-2H-1,2-benzo-(or -thieno-)thiazine-3-carboxamide 1,1-dioxide derivatives, compositions, and method of use therefor

Certain enol ether derivatives of oxicams (1,1-dioxides of N-heteroaryl-4-hydroxy-2-methyl-2H-1,2-benzothiazine-3-carboxamides and N-heteroaryl-4-hydroxy-2-methyl-2H-thieno[2,3-e]-1,2-thiazine-3-carboxamides) are useful as prodrugs of these antiinflammatory compounds.