Alanine, Alexander et al. published their patent in 2001 |CAS: 124038-36-4

The Article related to nmda receptor blocking triazole imidazole derivative preparation, glutamate receptor nmda binding blocking triazole imidazole derivative preparation, Heterocyclic Compounds (More Than One Hetero Atom): Other 5-Membered Rings, Two Or More Hetero Atoms and other aspects.Application of 124038-36-4

On January 24, 2001, Alanine, Alexander; Buettelmann, Bernd; Heitz, Neidhart Marie-Paule; Jaeschke, Georg; Pinard, Emmanuel; Wyler, Rene published a patent.Application of 124038-36-4 The title of the patent was Triazole and imidazole derivatives, methods of preparation and use in treatment or prophylaxis of diseases caused by overactivation of respective NMDA receptor subtypes. And the patent contained the following:

The present invention relates to I wherein R1-R4 = H, CF3, OCF3, OCHF2, OCH2F, lower alkyl, lower alkoxy, halogen, hydroxy, Ph, benzyl, amino, nitro, pyrrol-1-yl, lower alkylsulfonyl, lower alkylthio, cyano or benzyloxy; or R2 and R3 may be together = O-(CH2)2-O-, -O-CH2-O-, -O-(CH2)2-, -(CH2)3- or CH:CH-CH:CH-; X = N:, imino with N possibly substituted, CH:; Y = -N:, :N-, imino with N possibly substituted, CH:; wherein one of X or Y has to be N; R5 = aminomethyl with N possibly substituted and to their pharmaceutically acceptable acid addition salts. The methods of preparation comprise cyclizing a carboxylic acid hydrazide with a benzenecarboximidamide hydrochloride or benzenecarboximidic acid ester to give a triazole; arylating a 4-iodo-2-phenylimidazole with a phenylboronic acid in the presence of Pd(PPh3)4 to give an imidazole; reducing II to the aminomethyl analog followed by di-N-alkylation using acyl chlorides and LiAlH4. These compounds may be used for the treatment or prophylaxis of diseases related to the N-methyl-D-aspartate (NMDA)-receptor-subtype selective blockers. Such diseases include acute forms of neurodegeneration caused, e.g., by stroke or brain trauma; chronic forms of neurodegeneration such as Alzheimer’s disease, Parkinson’s disease, Huntington’s disease or ALS (amyotrophic lateral sclerosis); neurodegeneration associated with bacterial or viral infections, and diseases such as schizophrenia, anxiety, depression and acute/chronic pain. The experimental process involved the reaction of Methyl 3-(1,3-dioxolan-2-yl)benzoate(cas: 124038-36-4).Application of 124038-36-4

The Article related to nmda receptor blocking triazole imidazole derivative preparation, glutamate receptor nmda binding blocking triazole imidazole derivative preparation, Heterocyclic Compounds (More Than One Hetero Atom): Other 5-Membered Rings, Two Or More Hetero Atoms and other aspects.Application of 124038-36-4

Referemce:
1,3-Benzodioxole – Wikipedia,
Dioxole | C3H4O2 – PubChem