Delving into the Latest Updates on Chinoin Zrt. with Synapse

Overview

A new Pd/MgLa mixed oxide and the known Pd/MgAl hydrotalcite catalysts were applied and recycled successfully in catalytic transfer hydrogenation reactions in ionic liquidsSome α,β-unsaturated carboxylic acid derivatives were hydrogenated in excellent yields.The catalysts were recycled without significant loss of activity.Besides that, a number of halogenated aromatic compounds were dehalogenated under similar catalytic transfer conditions.

01 Oct 2001·The Journal of Organic ChemistryQ2 · CHEMISTRY

Novel Intramolecular Rearrangement of Tertiary PropargylamineN-Oxides

Q2 · CHEMISTRY

Article

Author: Hermecz, István ; Szabó, Anna

The formation of enamino aldehydes and acrylamides from tertiary propargylamine N-oxides in protic media can be interpreted as a novel prototropic rearrangement.The proposed rearrangement mechanism is supported by isotopic labeling experiments and by relevant literature data.

01 Sep 2001·Pure and Applied Chemistry

Chemical development of the vasopressin receptor 2 antagonist SR-121463

Author: Podányi, Benjámin ; Simon, Kálmán ; Hermecz, István ; Csikós, Éva ; Smelkó-Esek, Ágota ; Sánta-Csutor, Andrea ; Gönczi, Csaba ; Héja, Gergely

AbstractA facile convergent total synthesis of the selective, potent, and orally active V2 non-peptide antagonist, SR-121463, was developed by modification of the discovery route. One of the late intermediates, the sulfonyl chloride 1, was synthesized from 3-hydroxybenzoic acid (19) by regioselective sulfonation, O-methylation and amidation in four steps. Another late intermediate, indolin-2-one 2, was prepared from p-phenetidine (8) through the indolin-2-one 16, where the cyclohexanone moiety of 27 was introduced into the active 3-methylene group of 16 by sequential transformation using methyl acrylate and KOtBu. After formation of the cyclic ketal moiety of 13, its ring-opening was achieved by using NaBH4 in the presence of CCl3COOH. The morpholino group in 2 was introduced in accordance with the discovery approach, starting from the 2-hydroxyethoxy derivative 14 through the tosyloxy derivative 15 with morpholine in a one-pot reaction. In this way, the indolin-2-one 2 was synthesized from 8 in six steps. Finally, acylation of the indolin-2-one 2 was achieved with the sulfonyl chloride 1 in the presence of KOtBu in dimethyl sulfoxide (DMSO) at room temperature. This synthetic route proved to be applicable for the large-scale synthesis of SR-121463.

100 Deals associated with Chinoin Zrt.

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100 Translational Medicine associated with Chinoin Zrt.

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Pipeline

Pipeline Snapshot as of 26 Nov 2024

The statistics for drugs in the Pipeline is the current organization and its subsidiaries are counted as organizations,Early Phase 1 is incorporated into Phase 1, Phase 1/2 is incorporated into phase 2, and phase 2/3 is incorporated into phase 3

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Current Projects

Drug(Targets)	Indications	Global Highest Phase

KHL-9114 ( CaM )	Respiration Disorders More	Discontinued
CH-38083 ( α2A-AR )	Depressive Disorder, Major More	Discontinued
Acitemate ( HMG-CoA reductase )	Hyperlipidemias More	Discontinued
Drotaverine acephyllinate ( nAChRα1/β1/δ/γ )	Peripheral Vascular Diseases More	Discontinued
Chinoin 127	Peptic Ulcer More	Discontinued