32012-12-7

Usage

Uses

Used in Pharmaceutical Industry:
N~1~-methylalaninamide(SALTDATA: HCl) is used as a reagent for the acetylation of DL-amino acid derivatives, which are potent new agents for the treatment of epilepsy. Its role in the synthesis of these agents is crucial, as it helps in the development of more effective and targeted therapies for epilepsy patients.
In the development of new antiepileptic drugs, N~1~-methylalaninamide(SALTDATA: HCl) plays a significant role in the acetylation process, which is essential for enhancing the therapeutic effects of the resulting compounds. This allows for the creation of more potent and selective treatments that can better manage the symptoms and progression of epilepsy.

Upstream product

• 38215-69-9 (1-Methylcarbamoyl-vinyl)-carbamic acid benzyl ester 
• 17344-99-9 AlaOEt 
• 74-89-5 methylamine 
• 13515-97-4 methyl 2-aminopropanoate monohydrochloride 
• 88815-86-5 Boc-Ala-NHMe 

Relevant academic research and scientific papers

Amine derivative, and preparation method and medical application thereof

The present invention relates to a compound represented by formula (I), or a stereoisomer, a pharmaceutically acceptable salt and a medical use thereof. The compound shown in the formula (I) can be effectively combined with BRD4, and can be used as a BRD4 inhibitor for treating various diseases related to BRD4.

Bioinspired Radical Stetter Reaction: Radical Umpolung Enabled by Ion-Pair Photocatalysis

A bioinspired, intermolecular radical Stetter reaction of α-keto acids and aldehydes is disclosed that is contingent on a formal “radical umpolung” concept. Enabled by secondary amine activation, electrostatic recognition ensures that the α-ketocarboxylic acids, which function as latent acyl radicals, are proximal to the in situ generated iminium salts. This photoactive contact ion pair is an electron donor–acceptor (EDA) complex, and undergoes facile single electron transfer (SET) and rapid decarboxylation prior to radical–radical recombination. Importantly, decarbonylation is mitigated by this strategy. The initial computational validation on which the process is predicated matches closely with experiment. Synergising organo- and photocatalysis activation principles finally expands the mechanistic and synthetic scope of the classic Stetter reaction to include α,β-unsaturated aldehydes as acceptors.

NEW SUBSTITUTED ARYLSULPHONYLGLYCINES, THE PREPARATION THEREOF AND THE USE THEREOF AS PHARMACEUTICAL COMPOSITIONS

The present invention relates to substituted arylsulphonylglycines of general formula (I) wherein R, X, Y and Z are defined as in claim 1, the tautomers, enantiomers, diastereomers, mixtures thereof and salts thereof, which have valuable pharmacological properties, particularly the suppression of the interaction of glycogen phosphorylase a with the GL subunit of glycogen-associated protein phosphatase 1 (PP1 ), and their use as pharmaceutical compositions.

IRON MODULATORS

Iron modulator compounds of formula (I) are provided for treating amyloidoses wherein R1 is selected from H, C1-6 alkyl, C1-6 alkenyl, C1-6 hydroxyalkyl, C1-6 hydroxyalkenyl, R2 is selected from H, C1-6 alkyl, C1-6 alkenyl, C1-6 hydroxyalkyl, C1-6 hydroxyalkenyl and C6-10 aralykyl in which the aryl group of the aralkyl group is optionally substituted by hydroxy, halo or C1-4 alkyl R3 is selected from H, C1-6 alkyl, C1-6 alkenyl and C1-12 acyl; R4 is selected from H and C1-3 alkyl R5, R6 and R7 are independently selected from H, C1-6 alkyl, C3-7 aryl, and C1-10 aralkyl; the alkyl, aryl and aralkyl groups being optionally substituted by one or more halo, hydroxy and nitro groups or R5 and R7 together with the nitrogen atom to which they are bonded form a heterocyclic ring optionally substituted by one or more hydroxyl groups or a pharmaceutically acceptable tautomer, ester or addition salt thereof.

Functionalized DL-Amino Acid Derivatives. Potent New Agents for the Treatment of Epilepsy

Structural analogues of the potent known anticonvulsant agent N-acetyl-DL-alanine N-benzylamide (1a) have been prepared (16 examples).The pharmacological activities of these products were evaluated in the maximal electroshock seizure (MES), the subcutaneous pentylenetetrazole seizure threshold (sc Met), and the rotorod (Tox) tests.The median effective doses (ED50) and the median toxic doses (TD50) for the most active compounds by both intraperitoneal and oral administration are reported.The most active compounds were N-acetyl-DL-phenylglycine N-benzylamide (1d) and N-acetyl-DL-alanine N-m-fluorobenzylamide (1m) along with the parent compound 1a.The ED50 values in the MES test for these three compounds compared well with phenobarbital, while their high TD50 values contributed to their large protective indexes, which approached that of phenytoin.When tested against four convulsant agents, compounds 1a and 1d displayed activity profiles significantly different from those reported for conventionally used antiepileptic drugs.