Basilea Pharmaceutical China Ltd.

Jiaojiang, China

Basilea Pharmaceutical China Ltd.

Jiaojiang, China
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Zhang J.,Shanghai University of Traditional Chinese Medicine | Zheng S.,Basilea Pharmaceutical China Ltd. | Peng W.,Basilea Pharmaceutical China Ltd. | Shen Z.,Shanghai University of Traditional Chinese Medicine | Shen Z.,Basilea Pharmaceutical China Ltd.
Tetrahedron Letters | Year: 2014

A novel and efficient total synthesis of Englerin A is reported. The synthesis featured an intramolecular olefin metathesis ring closure reaction and a highly stereoselective oxygen bridge formation induced by an iodonium ion. This strategy can be used for the synthesis of natural products Englerin A and Englerin B and can provide flexibility in the preparation of various 9-substituted analogues of Englerin A for further structure-activity relationship studies. © 2014 Elsevier Ltd. All rights reserved.


Zheng S.,Shanghai University of Traditional Chinese Medicine | Tan H.,Shanghai University of Traditional Chinese Medicine | Zhang X.,Shanghai University of Traditional Chinese Medicine | Yu C.,Shanghai University of Traditional Chinese Medicine | And 2 more authors.
Tetrahedron Letters | Year: 2014

A novel one-pot thermal cycloaddition of two indenones followed by a decarbonylation and dehydrogenation cascade afforded benzo[c]fluorenones regioselectively. Various substituted indenone derivatives were converted into their corresponding benzo[c]fluorenones in good to excellent yields. © 2013 Elsevier Ltd. All rights reserved.


Zheng S.,Shanghai University of Traditional Chinese Medicine | Yu C.,Shanghai University of Traditional Chinese Medicine | Shen Z.,Shanghai University of Traditional Chinese Medicine | Shen Z.,Basilea Pharmaceutical China Ltd.
Chinese Journal of Organic Chemistry | Year: 2013

Huperzine A has been widely used for the treatment of alzheimer in China, and has attracted widespread attention. It has been entered into phase 3 investigation in US and phase 4 investigation in China for the treatment of alzheimer and related disease. Due to the trace content in the herb Huperzia serrata, the chemical synthesis of huperzine A becomes the attractive option for drug supply. During the past two decades, significant progresses have been achieved for the stereoselective synthesis of (-)-huperzine A. The total synthesis of hundreds of grams of (-)-huperzine A has been achieved recently. In addition to the efficiency of the synthesis, the safety of the process was also significantly improved. The progresses of the total synthesis of huperzine A made from 1989 to 2013 are comprehensively reviewed in this paper. © 2013 Chinese Chemical Society & SIOC, CAS.


Shou Q.-Y.,Shanghai University of Traditional Chinese Medicine | Tan Q.,Shanghai University of Traditional Chinese Medicine | Shen Z.,Shanghai University of Traditional Chinese Medicine | Shen Z.,Basilea Pharmaceutical China Ltd.
Planta Medica | Year: 2010

From the dried roots of Campylotropis hirtella (Franch.) Schindl., five novel isoflavonoids, 3(S)-7,2,4-trihydroxy-5,5-dimethoxy-6-(3-methylbut-2-enyl)- isoflavan (1), 3(S)-2,4-dihydroxy-5,5-dimethoxy-(6,6-dimethylpyrano)-(2,3:7,6)- isoflavan (2), 3(R)-5,4-dihydroxy-2-methoxy-3-(3-methylbut-2-enyl)-(6,6- dimethylpyrano)-(7,6:2,3)-isoflavanone (3), 3(R)-5,4-dihydroxy-2-methoxy-(6,6- dimethylpyrano)-(7,6: 2,3)-isoflavanone (4), and 3(R)-5,4-dihydroxy-7,2- dimethoxy-6-geranylisoflavanone (5) were isolated. The structures of the compounds were elucidated on the basis of spectroscopic analysis. All isolates exhibited good immunosuppressive activities on mitogen-induced splenocyte proliferation, and their cytotoxicity on splenic lymphocytes was also tested. © Georg Thieme Verlag KG Stuttgart · New York.


Zheng S.-Y.,Shanghai University of Traditional Chinese Medicine | Li X.-P.,Shanghai University of Traditional Chinese Medicine | Tan H.-S.,Shanghai University of Traditional Chinese Medicine | Yu C.-H.,Shanghai University of Traditional Chinese Medicine | And 3 more authors.
European Journal of Organic Chemistry | Year: 2013

The total synthesis of Hirtellanine A was accomplished by two different synthetic approaches. Hirtellanine A was assembled using a one-pot, tandem acid-mediated deprotection and tautomerization cascade starting from quinone derivative 23. The key features of the synthesis include a Houben-Hoesch reaction of aryl cyanide 3 with phloroglucinol, a one-pot sequential boronation, a Suzuki-Miyaura cross-coupling of aryl bromide 33 with aryl iodide 26, and a base-mediated regioselective Claisen rearrangement for the benzopyran construction. The total synthesis of Hirtellanine A was achieved. The synthesis featured a one-pot, tandem acid-mediated deprotection and tautomerization cascade for the construction of the coumaronochromone motif, and a regioselective Claisen rearrangement for the benzopyran construction. Copyright © 2013 WILEY-VCH Verlag GmbH & Co. KGaA, Weinheim.

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