Allist Pharmaceuticals Inc.

Shanghai, China

Allist Pharmaceuticals Inc.

Shanghai, China
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Wang Y.,China Pharmaceutical University | Zhang Y.,Allist Pharmaceuticals Inc. | Yang B.,China Pharmaceutical University | Zhang A.,CAS Shanghai Institute of Materia Medica | Yao Q.,China Pharmaceutical University
Organic and Biomolecular Chemistry | Year: 2015

N-(1-Oxy-pyridin-2-ylmethyl)oxalamic acids (L3-L5) were identified as novel efficient ligands for copper-catalyzed C-N cross-coupling of azoles and aryl halides in water. The N-arylation of imidazoles, indoles and pyrazoles proceeded with moderate to excellent yields and complete selectivity over aromatic amines and phenols. Moreover, L5, which is also efficient in organic solvent with low catalyst loading, can be used to promote the N-arylation reactions with water-sensitive materials. The catalytic mechanism was proposed based on the results of several verification experiments which indicated that the ligands as new-type chelators may coordinate to Cu(i) with two oxygen atoms of N-oxide and amide in the coupling process. This journal is © The Royal Society of Chemistry 2015.


Wang Y.,China Pharmaceutical University | Ling J.,China Pharmaceutical University | Zhang Y.,Allist Pharmaceuticals Inc. | Zhang A.,CAS Shanghai Institute of Materia Medica | Yao Q.,China Pharmaceutical University
European Journal of Organic Chemistry | Year: 2015

N-(1-Oxy-pyridin-2-ylmethyl)oxalamic acid was identified as efficient ligand for CuI-catalyzed amination of aryl halides at room temperature. In our catalytic system, N-arylation of cyclic secondary amines, primary amines, amino acids, and ammonia proceeded with moderate to excellent yields and high functional group tolerance. © 2015 WILEY-VCH Verlag GmbH & Co. KGaA, Weinheim.


Meng X.,Zhejiang University | Lu F.,Zhejiang University | Lu F.,Allist Pharmaceuticals Inc. | Zhao H.,Zhejiang University
Acta Chimica Sinica | Year: 2011

In this paper, a simple, environment-friendly and efficient one-pot way to synthesize 2-amino-4-thiazolinones at room temperature was reported. Ethyl 2-thiocyanatoacetate was formed by substitution reaction of ethyl chloroacetate with thiocyanate in [Bmim]SCN. After that, when HOAc was employed as a catalyst, 2-amino-4-thiazolinones were produced in high yields through the nucleophilic attack of amines to ethyl 2-thiocyanatoacetate following ring-closing reaction of intermediate product S-alkyl isothioureas. As a task-specific ionic liquid, [Bmim]SCN plays a role of a solvent as well as a reactant. And it can be recycled. The crystal structure of 2-(4-ethylpiperzin-1-yl)-4-thiazolinone (3i) was confirmed by X-ray diffraction study.

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