120686-09-1Relevant articles and documents
Synthesis method of 2-methoxy-7,8-dihydroquinoline-6(5H)-ketone
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Paragraph 0034-0036, (2018/03/26)
The invention relates to the technical field of chemical synthesis processes of tetrahydroquinoline derivatives, in particular to a synthesis method of 2-methoxy-7,8-dihydroquinoline-6(5H)-ketone. Inthe method, 1,4-cyclohexanedione monoethylene glycol is
A 2-methoxy-6-one -5, 6, 7, 8-tetrahydro-quinoline synthesis method
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Paragraph 0042-0045, (2017/02/17)
The invention discloses a synthesis method of a drug intermediate 2-methoxy-6-one-5,6,7,8-tetrahydroquinoline. 1,4-cyclohexyldione monoethylene ketal used as the raw material is subjected to five-step reaction to generate the important intermediate 2-meth
Reversible acetylcholinesterase inhibitor huperzine-A synthesis method
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Paragraph 0231; 0232; 0233, (2017/02/23)
The present invention discloses a reversible acetylcholinesterase inhibitor huperzine-A synthesis method, wherein the route is defined in the specification. The method of the present invention has advantages of easily-available raw materials, simple operation, high yield, low cost, high purity of the final product, easy quality control and the like, and is suitable for industrial production.
FUSED PYRIDINE AND PYRIMIDINE DERIVATIVES AS ROR GAMMA MODULATORS
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Page/Page column 54.iii, (2015/06/18)
The present invention provides fused pyridine and pyrimidine derivatives of formula (I), which may be therapeutically useful, more particularly as RORγ modulators; in which Ra, Rb, A, B, X, P, Q, L, R4, R5 and m
Development of a large-scale synthetic route to manufacture (-)-huperzine A
Tudhope, Stephen R.,Bellamy, Julie A.,Ball, Anthony,Rajasekar, Dewakar,Azadi-Ardakani, Manouchehr,Meera, Harihara Subramanian,Gnanadeepam, Jesudoss Mercy,Saiganesh, Ramanathan,Gibson, Frank,He, Linli,Behrens, Carl H.,Underiner, Gail,Marfurt, Judith,Favre, Nathalie
experimental part, p. 635 - 642 (2012/07/28)
A safe, practical and scalable process for manufacture of (-)-huperzine A has been developed and scaled up to manufacture several hundred grams of (-)-huperzine A with chemical and optical purity of >99%. The process consists of 11 chemical stages starting from commercially available materials with only nine isolation steps and no chromatography purification. This process provides a reliable and cost-effective source of synthetic (-)-huperzine A and its derivatives for pharmaceutical and nutraceutical markets.
Target-oriented multifunctional organocatalysis for enantioselective synthesis of bicyclo[3.3.1]nona-2,6-dien-9-ones. A formal asymmetric synthesis of huperzine A
Ding, Xiao-Hua,Li, Xiang,Liu, Dan,Cui, Wei-Chen,Ju, Xuan,Wang, Shaozhong,Yao, Zhu-Jun
experimental part, p. 6240 - 6248 (2012/08/28)
A target-oriented highly enantioselective multifunctional organocatalytic approach has been developed to construct the bicycle-[3.3.1]nona-2,6-dien-9-one core of (-)-huperzine A for the first time, with up to 95% ee in the gram-scale procedure. The newly established methodology is also eligible to synthesize a variety of bicyclo[3.3.1]nona-2,6-dien-9-ones in high enantiopurities, and thus is useful for the future development of novel huperzine A analogs with medicinal interests.
METHOD OF PREPARING HUPERZINE A AND DERIVATIVES THEREOF
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Page/Page column 10; 7, (2009/10/06)
The present invention is related to the synthesis of huperzine A. The synthesis includes a variety of process steps that increase productivity, reduce safety concerns, and allow for increasing production of compounds of desired optical isomer. The inventive methods may encompass a single improved reaction step that may be incorporated into a known reaction process for synthesizing huperzine A or a derivative thereof to improve the overall reaction. The inventive methods also encompass complete synthesis methods for preparing huperzine A or a derivative thereof.
Racemic huperzine A
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Page 16, (2010/11/29)
The present invention relates to racemic huperzine A, a pharmaceutical composition comprising huperzine A, its use as a medicament and for the manufacture of a medicament for the inhibition of the cholesterase enzymes in a mammal.
Synthesis of a hybrid analog of the acetylcholinesterase inhibitors huperzine A and huperzine B
Rajendran,Rong, Suo-Bao,Saxena, Ashima,Doctor, Bhupendra P.,Kozikowski, Alan P
, p. 5359 - 5361 (2007/10/03)
The synthesis of a new hybrid analog of the acetylcholinesterase (AChE) inhibitors huperzine A and B is reported. An intramolecular reductive dicarbonyl coupling was used as a key reaction for constructing the tetracyclic ring system.
Synthesis and dopaminergic activity of pyridine analogs of 5-hydroxy-2- (di-n-propylamino)tetralin
Glase,Corbin,Pugsley,Heffner,Wise
, p. 3132 - 3137 (2007/10/03)
The pyridine analogs of 5-hydroxy-2-(di-n-propylamino)tetralin (5-OH- DPAT), 4-6, were synthesized, and their biological activity was compared to that of 5-OH-DPAT. Compounds 4 and 6 exhibited activity similar to 5-OH-DPAT in dopamine (DA) D2 a