105779-71-3

Upstream product

• 127095-97-0 (2S)-2-[(tert-butoxycarbonyl)amino]-3-(3,4-dimethoxyphenyl)propanoic acid 
• 30033-24-0 (2S)-3-(3,4-dihydroxyphenyl)-2-[(tert-butoxy)carbonylamino]propanoic acid 
• 59-92-7 levodopa 
• 32161-30-1 (S)-3,4-dimethoxyphenylalanine 
• 24424-99-5 di-tert-butyl dicarbonate 
• 138908-56-2 (S)-(+)-2-tert-butoxycarbonylamino-3-(3,4-dimethoxyphenyl)propionic acid methyl ester 
• 80582-39-4 (2S)-2-amino-3-(3,4-dimethoxyphenyl)-1-propanol 

Downstream Products

• 872516-06-8 (S)-(-)-[1-(methoxymethyl)-2-(3,4-dimethoxyphenyl)ethyl]carbamic acid tert-butyl ester 
• 142763-11-9 (S)-4-(3,4-dimethoxybenzyl)oxazolidin-2-one 
• 1394175-08-6 rac-8-(3,4-dimethoxybenzyl)-7,8-dihydroimidazo[1,2-a]pyrazin-6-one 
• 1394175-05-3 [rac-2-(3,4-dimethoxyphenyl)-1-(1H-imidazol-2-yl)ethyl]carbamic acid tert-butyl ester 
• 1394175-04-2 tert-butyl (S)-(1-(3,4-dimethoxyphenyl)-3-oxopropan-2-yl)carbamate 
• 1203464-18-9 (S)-3-(3,4-dihydroxyphenyl)-2-(N-methylamino)-propan-1-ol hydrobromide 
• 1203464-16-7 (R)-N-methyl-α-methyldopamine hydrobromide 
• 1203464-15-6 (S)-3-(3,4-dimethoxyphenyl)-2-(N-methylamino)propan-1-ol 
• 138908-40-4 CL 316243 
• 139013-14-2 5-{(R)-2-[(R)-5-(3-Chloro-phenyl)-2-oxo-oxazolidin-3-yl]-propyl}-benzo[1,3]dioxole-2,2-dicarboxylic acid diethyl ester 
• 138908-58-4 [R-(R*,R*)]-5-(3-chlorophenyl)-3-[2-(3,4-dimethoxylphenyl)-1-methyl-ethyl]-oxazolidin-2-one 
• 142796-56-3 (R)-5-(3-Chloro-phenyl)-3-[(R)-2-(3,4-dihydroxy-phenyl)-1-methyl-ethyl]-oxazolidin-2-one 
• 142796-55-2 (R)-1-(3-Chloro-phenyl)-2-[(R)-2-(3,4-dimethoxy-phenyl)-1-methyl-ethylamino]-ethanol 

Relevant academic research and scientific papers

Oxidative nucleophilic substitution (SNOX) of the benzylic position as a tunable synthesis of tetrahydroisoquinoline natural alkaloid analogues

Synthetic investigations of 1,3-dichloro-5,6-dicyanobenzoquinone-mediated benzylic oxidation is reported for the synthesis of natural alkaloid analogues. Extensive explorations of the oxidative nucleophilic substitution of the benzylic position of β-phenylethylamine derivatives and the synthesis of functionalized tetrahydroisoquinolines of ecteinascidin 743 precursors have been carried out. Starting from L-DOPA, a tunable oxazolidinone group was installed under oxidative benzylic conditions. This derivative 13 was submitted to benzylic oxidation reactions using a wide range of carboxylic acids and subsequent chemical transformations of these compounds were attempted. Moreover, an efficient synthesis of an aromatic ketone derivative 20 was achieved and gave rise to tetrahydroisoquinoline 24 through a direct Pictet-Spengler cyclisation reaction. Subsequently, 24 was transformed into functionahzed α-amino alcohols 31a and 31b, precursors of ecteinascidin 743 analogues. In addition, in order to assess the viability of our synthetic strategy, the reaction of 24 with methyl thioglycolate was performed and the stereoselectivity confirmed by X-ray analysis of 33a. Wiley-VCH Verlag GmbH & Co. KGaA, 2007.

Synthesis and Biological Evaluation of Endocannabinoid Uptake Inhibitors Derived from WOBE437

WOBE437 ((2E,4E)-N-(3,4-dimethoxyphenethyl)dodeca-2,4-dienamide, 1) is a natural product-derived, highly potent inhibitor of endocannabinoid reuptake. In this study, we synthesized almost 80 analogues of 1 with different types of modifications in the dodecadienoyl domain as well as the dimethoxyphenylethyl head group, and we investigated their effects on anandamide uptake into U937 cells. Intriguingly, none of these analogues was a more potent inhibitor of anandamide uptake than WOBE437 (1). At the same time, a number of WOBE437 variants exhibited potencies in the sub-100 nM range, with high selectivity over inhibition of the endocannabinoid-degrading enzyme fatty acid amide hydrolase; two compounds were virtually equipotent with 1. Interestingly, profound activity differences were observed between analogues in which either of the two methoxy substituents in the head group had been replaced by the same bulkier alkoxy group. Some of the compounds described here could be interesting departure points for the development of potent endocannabinoid uptake inhibitors with more drug-like properties.

Nitrogen (oxygen) heterocyclic pentane - 2 - one (thione) compound, pharmaceutical composition, preparation method and use thereof

The invention belongs to the field of pharmacology, and relates to aza (oxa)-cyclopentane-2- ketone (thione) compounds shown in the formula I, medicine compositions thereof, a preparation method, applications in preparation of medicines treating diabetes and glucolipid metabolism, and especially applications in preparation of medicines treating II-type diabetes.

NOVEL INDOLE AND PYRROLOPYRIDINE AMIDES

The present invention relates to indole and pyrrolopyridine amide derivatives of formula (I) wherein R1, R 2, R 3, U, V, W, X, Y, Z and ring A are as described in the description, to their preparation, to pharmaceutically acceptable salts thereof, and to their use as pharmaceuticals, to pharmaceutical compositions containing one or more compounds of formula (I), and especially to their use as orexin receptor antagonists.

Synthesis and in vitro cytotoxicity profile of the R-enantiomer of 3,4-dihydroxymethamphetamine (R-(-)-HHMA): Comparison with related catecholamines

(±)-3,4-Methylenedioxymethamphetamine (MDMA, also known as "ecstasy") is a chiral drug that is essentially metabolized in humans through O-demethylenation into 3,4-dihydroxymethamphetamine (HHMA). There has recently been a resurgence of interest in the po

Diastereoselective intramolecular α-amidoalkylation reactions of L-DOPA derivatives. Asymmetric synthesis of pyrrolo[2,1-a]isoquinolines

Stereocontrolled intramolecular α-amidoalkylation reactions of L-DOPA-derived succinimides have been studied. Addition of MeLi to nonracemic succinimides 9a-d yields oxoamides, which are cyclized upon treatment with Lewis or protic acids to afford (5S,10b

Enantioselective synthesis of pyrrolo[2,1-a]isoquinolones via stereocontrolled N-acyliminium ion cyclisations

Stereocontrolled N-acyliminium ion cyclisation of L-DOPA derived succinimide 5 has been investigated. Addition of organolithiums to chiral non-racemic 5 yields oxoamides, which are cyclised diastereoselectively upon treatment with BF3·OEt2, to afford 5,10b-trans pyrroloisoquinolones in moderate yields and high ee (99%).

Method of increasing lean meat in edible animals

The present invention discloses substituted 1,3-benzodioxoles which possess anti-diabetic and/or anti-hyperglycemic and/or anti-obesity properties in humans and other animals.

Substituted 5-(2-((2-aryl-2-hydroxyethyl)amino)propyl)-1,3-benzodioxoles

The present invention discloses substituted 1,3-benzodioxoles which possess anti-diabetic and/or anti-hyperglycemic and/or anti-obesity properties in humans and other animals.