4801-39-2

Usage

InChI:InChI=1/C8H10N2O.ClH/c1-6(11)10-8-5-3-2-4-7(8)9;/h2-5H,9H2,1H3,(H,10,11);1H

Upstream product

• 6833-09-6 benzyl (2-oxo-2-(phenylamino)ethyl)carbamate 
• 27904-92-3 N-glycyl>aniline 
• 611-71-2 MANDELIC ACID 
• 21969-70-0 2-anilinoacetamide 
• 62-53-3 aniline 
• 42366-35-8 hydroxyimino-N-phenylacetamide 

Downstream Products

• 67863-08-5 2-phenyl-[1,2,5]thiadiazol-3-one 
• 103565-85-1 N-alanyl-glycine anilide 
• 73376-17-7 PhCH₂O-DL-Ala-Gly-NHPh 
• 98554-96-2 N-phenyl-α-diazoacetamide 
• 17202-89-0 1-Spiro<2,5>octan-carbonsaeure-anilid 
• 93545-73-4 (Z)-7-{(1S,2R,3R,4R)-3-[(Phenylcarbamoylmethyl-amino)-methyl]-7-oxa-bicyclo[2.2.1]hept-2-yl}-hept-5-enoic acid 
• 68876-14-2 4-chloro-2-phenyl-[1,2,5]thiadiazol-3-one 

Relevant academic research and scientific papers

NovelN-transfer reagent for converting α-amino acid derivatives to α-diazo compounds

A novel universalN-transfer reagent for direct and effective transformation of α-amino ketones, acetamides, and esters to the corresponding α-diazo products under mild basic conditions has been developed. This one-step synthetic approach not only allows for generation of α-substituted-α-diazo carbonyl compounds from α-amino acid derivatives but also permits preparation of α-diazo dipeptides fromN-terminal dipeptides (32 examples, up to 91%).

N-transfer reagent and method for preparing the same and its application

Provided are a novel N-transfer reagent and a method for preparing the same and its application. The N-transfer reagent is represented by the following Formula (I): The various novel N-transfer reagents of the present invention can be quickly prepared by employing different nitrobenzene precursors. The N-transfer reagents can directly convert a variety of amino compounds into diazo compounds under mild conditions. Particularly, the N-transfer reagents can facilitate the synthesis of the diazo compounds. The application of synthesizing diazo compounds of the present invention can greatly decrease the difficulty in operation, increase the safety during experiments, reduce the cost of production and the environmental pollution, and enhance the industrial value of diazo compounds.

2-substituted-4-site functionalized N (O, S)-quinazoline derivative and application thereof

The invention relates to the technical field of medicine synthesis, and provides a 2-substituted-4-site functionalized N (O, S)-quinazoline derivative and an application thereof. The 2-substituted-4-site functionalized N (O, S)-quinazoline derivative prov

Design, synthesis and in vitro anti-influenza A virus evaluation of novel quinazoline derivatives containing S-acetamide and NH-acetamide moieties at C-4

It is an urgent need to develop more effective anti-influenza agents due to the emergence of highly pathogenic and drug-resistant influenza viruses. Herein, a series of 2,4-disubstituted quinazoline derivatives were designed, synthesized and their antiviral activities against influenza A virus were evaluated. Nine compounds (10a2, 16a, 16e, 16i, 16j, 16n, 16o, 16p and 16r) showed potent activity against influenza A virus (IAV) with IC50 at the low-micromole level (1.29–9.04 μM). Particularly, 16e and 16r possess good anti-IAV activity (IC50: 1.29 μM and 3.43 μM, respectively) and acceptable cytotoxicity, and inhibit the transcription and replication of viral RNA. Together with reasonable PK profiles of 16e, these results suggest their promising potential as candidates for further investigation.

Process for preparation of an optically active amino acid amide

The present invention relates to a process for the preparation of optically active amino acid amide. L-amino and D-amino acid amides are mixed in the presence of 0.5-4 equivalents of an aldehyde, relative to the quantity of amino acid amide, in the presen

Process for racemization of an optically active amino acid amide

Process for the racemization of an optically active amino acid amide by reacting the amino acid amide with a carboxylic acid in the presence of a solvent, of water and of 0.5-4 equivalents of an aldehyde, calculated relative to the quantity of amino acid

N-N-DISUBSTITUTED-OMEGA-(2-AMINO-3-(CARBONYLMETHYL)-3,4-DIHYDROQUINAZOLINYL)OXY-ALKYLAMIDES AND RELATED COMPOUNDS

Compounds are disclosed according to the formula or an optical isomer thereof. The compounds of formula I are cyclic AMP phosphodiesterase inhibitors useful as antithrombotic and inotropic agents and the like in mammals

N-N-disubstituted-ω-[2-amino-3-(carbonylmethyl)-3, 4-dihydroquinazolinyl]oxyalkylamides and related compounds

Pharmaceutical compositions comprising, or compositions consisting essentially of, compounds according to the formula STR1 or an optical isomer thereof are disclosed, wherein the substituents A, Z and R1 are defined herein. The invention is also directed to certain compounds of the above class. The compounds of Formula I are cyclic AMP phosphodiesterase inhibitors useful as antithrombotic and inotropic agents and the like in mammals.

Inhibitors of Cyclic AMP Phosphodiesterase. 4. Synthesis and Evaluation of Potential Prodrugs of Lixazinone (N-Cyclohexyl-N-methyl-4quinazolin-7-yl)oxy>butyramide, RS-82856)

The cyclic AMP phosphodiesterase (cAMP PDE) inhibitor and cardiotonic agent lixazinone (N-cyclohexyl-N-methyl-4-quinazolin-7-yl)oxy>butyramide, RS-82856, 1) and its acid and base addition salts were found to be insufficiently soluble in formulations suitable for intravenous administration.These results prompted an investigation into potential prodrugs with enhanced aqueous solubility designed to deliver 1 by three distinct mechanisms: (1) decarboxylation of α-carboxamides; (2) hydrolytic loss of a solubilizing N-1-(acyloxy)methyl or (N,N-dialkylamino)methyl moiety; or (3) intramolecular closure of a guanidino ester or amide.The target compounds were evaluated as delivery systems for 1 by three criteria: (1) chemical conversion rate to 1 under physiological conditions; (2) inhibition of type IV cAMP PDE at a fixed time point; and (3) in vivo inotropic activity in anesthetized dogs by both intravenous and oral administration.Release of 1 from 4a (series 1) was found to be too slow to be of value as prodrug of 1, since decarboxylation could be induced only by strong acid, conditions under which hydrolytic ring opening was found to severely compete.Conversely, 1 was released too readily on exposure of (N,N-dialkylamino)methyl derivatives such as 8d (series 2) to physiological conditions, although no large increase in aqueous solubility was realized.Finally, both the physicochemical and in vitro studies indicated that ring closure of the guanidinium esters and amides 17a-k (series 3) to 1 was quantitative and pH- and time-dependent, suggesting the possibility of delivery of the open, water-soluble prodrug form, followed by closure to 1 in plasma.Detailed examination of these agents in vivo, however, demonstrated that only those compounds that rapidly cyclized to 1, as measured by plasma levels of 1, exhibited inotropic activity, indicating that the open prodrug form was not efficiently absorbed upon oral administration.

A Mechanism for bitter Taste Sensibility in Peptides

To estimate the steric distance between the bitter taste determinant sites in peptides, some cyclic dipeptides, amino acid anilides, amino acid cyclohexylamides, and benzoyl amino acids were synthesized and their tastes were evaluated.The diketopiperazine ring of cyclic dipeptides acted as a bitter taste determinant site due to its hydrophobicity.The steric distance between 2 sites was estimated as 4.1 Angstroem from the molecule models of cyclic dipeptides composed of typical amino acids in the bitter peptides.Due to the hypothesis of two bitter taste determinant sites, which bind with the bitter taste receptor via a "binding unit" and a "stimulating unit," a mechanism for the bitterness in peptides was postulated.