94930-46-8

Upstream product

• 124-38-9 carbon dioxide 
• 32347-92-5 α,α-dimethoxy-m-fluorotoluene 
• 107977-85-5 2-Fluoro-6-(3,4,4-trimethyl-oxazolidin-2-yl)-benzoic acid methyl ester 
• 717816-83-6 2-dimethoxymethyl-6-fluorobenzoic acid 
• 10345-76-3 N,N-diethyl 2-fluorobenzamide 
• 393-52-2 2-Fluorobenzoyl chloride 
• 456-48-4 3-Fluorobenzaldehyde 
• 776255-12-0 2-(3-Methoxy-2-methoxycarbonyl-phenyl)-3,4,4-trimethyl-4,5-dihydro-oxazol-3-ium 
• 586-38-9 3-Methoxybenzoic acid 
• 107977-65-1 2-(4,4-Dimethyl-4,5-dihydro-oxazol-2-yl)-6-methoxy-benzoic acid methyl ester 
• 107977-64-0 2-(4,4-Dimethyl-4,5-dihydro-oxazol-2-yl)-6-methoxy-benzoic acid 
• 73453-77-7 3-(4,4-dimethyloxazolin 2-yl)anisole 
• 445-29-4 o-fluoro-benzoic acid 
• 113232-65-8 N,N-Diethyl-2-fluoro-6-formyl-benzamide 

Downstream Products

• 94930-55-9 2-(Cyano-hydroxy-methyl)-6-fluoro-benzoic acid 
• 1198117-21-3 4-fluoro-3-oxo-2-(2-(pyridin-2-yl)ethyl)-N-(4-(trifluoromethoxy)benzyl)isoindoline-1-carboxamide 

Relevant academic research and scientific papers

Chiral Bicyclic Imidazole-Catalyzed Acylative Dynamic Kinetic Resolution for the Synthesis of Chiral Phthalidyl Esters

Utilizing a chiral bicyclic imidazole organocatalyst and adopting a continuous injection process, an alternative route has been developed for the efficient synthesis of chiral phthalidyl ester prodrugs via dynamic kinetic resolution of 3-hydroxyphthalides through enantioselective acylation (up to 99 % ee). The computational studies suggest a general base catalytic mechanism differing from the widely accepted nucleophilic catalytic mechanism. The structure analysis of the key transition states shows that the CH-π interactions and not the previously considered cation/π-π interactions between the catalyst and substrate is the dominant factor giving rise to the observed stereocontrol.

Synthesis and biological activity of n-butylphthalide derivatives

A series of n-butylphthalide derivatives were designed and synthesized. The in vitro activities of these compounds were evaluated by a resting tension of isolated rat thoracic aorta ring assay. Compounds 4g and 4i were found to be more active than n-butylphthalide.

NEW COMPOUNDS I/418

There is provided compounds of formula I, wherein R1 to R7 have meanings given in the description, which are useful in the prophylaxis and in the treatment of arrhythmias, in particular atrial and ventricular arrhythmias.

Discovery of (R)-9-ethyl-1,3,4,10b-tetrahydro-7-trifluoromethylpyrazino[2, 1-a]isoindol-6(2H)-one, a selective, orally active agonist of the 5-HT 2C receptor

Robust pharmaceutical treatment of obesity has been limited by the undesirable side-effect profile of currently marketed therapies. This paper describes the synthesis and optimization of a new class of pyrazinoisoindolone- containing, selective 5-HT2C agonists as antiobesity agents. Key to optimization of the pyrazinoisoindolone core was the identification of the appropriate substitution pattern and functional groups which led to the discovery of (R)-9-ethyl-1,3,4,10b-tetrahydro-7-trifluoromethylpyrazino[2,1-a] isoindol-6(2H)-one (58), a 5-HT2C agonist with > 300-fold functional selectivity over 5-HT2B and > 70-fold functional selectivity over 5-HT2A. Oral dosing of 58 reduced food intake in an acute rat feeding model, which could be completely reversed by a selective 5-HT2C antagonist and caused a reduction in body weight gain in a 4-day rat model.

1-fluoro, 4-fluoro, and 1,4-difluoro-2'-halo anthracycline antibiotics

Anthracycline antibiotics represented by the formula (I) STR1 wherein R is hydrogen or hydroxyl, one of X and Y is fluorine and the other is hydrogen or both X and Y are fluorine, and S is a 2-halo sugar moiety; pharmaceutical preparations containing the same; and a method for inhibiting the growth of mammalian tumors are disclosed.

1-fluoro, 4-fluoro, and 1,4-difluoro anthracycline anticancer antibiotics

Compounds represented by the formula (I) STR1 wherein R is hydrogen or hydroxyl, one of X and Y is fluorine and the other is hydrogen or both X and Y are fluorine, and Su is a hydrogen atom or a sugar moiety; where Su is a sugar moiety, the compounds are useful anticancer antibiotics; pharmaceutical preparations containing the antibiotics and a method for inhibiting the growth of mammalian tumors are also disclosed.

A NEW ROUTE TO 3-HYDROXYPHTHALIDES : APPLICATION TO THE SYNTHESIS OF RACEMIC DAUNOMYCINONE.

Lithiation (n-BuLi) of the (3'-methoxyphenyl) oxazoline (2a) occurs specifically at C2' and, following carboxylation (CO2/13CO2) and esterification, yields the phthalate derivative (e.g. 5a).Elaboration of the oxazoline-ring furnishes the related aldehyde

A HIGH-YIELDING SYNTHESIS OF 3-CYANOPHTHALIDES

Dehydration, with dicyclohexylcarbodiimide, of the cyanohydrins derived from the ring open tautomers of the 3-hydroxyphthalides (4) provides an efficient synthesis of 3-cyanophthalides (8a) and its derivatives (8b-f).

Synthesis of Functionalized Hydroxyphthalides and Their Conversion to 3-Cyano-1(3H)-isobenzofuranones. The Diels-Alder Reaction of Methyl 4,4-Diethoxybutynoate and Cyclohexadienes

Several methods have been used in the preparation of functionalized hydroxyphthalides.Metalation of N,N-diethyl-3-methoxybenzamide, followed by reaction with dimethylformamide and hydrolysis, furnished 3-hydroxy-4-methoxy-1(3H)-isobenzofuranone in 52perce