- Preparation method of levo-demethyl benzene ring nonyl ester hydrochloride
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The invention belongs to the technical field of medicine preparation, and discloses a preparation method of levo-demethylated benzene ring nonyl ester hydrochloride, the molecular formula of the levo-demethylated benzene ring nonyl ester hydrochloride is shown as (1), the method comprises the following steps: (1) preparing (R)-alpha-phenyl-alpha-cyclopentyl-alpha-methyl glycolate; (2) preparing anintermediate, wherein the intermediate is N-benzyl-3-azabicyclo-[3.3. 1]-non-9 [alpha]-alcohol; and (3) carrying out transesterification on the (R)-alpha-phenyl-alpha-cyclopentyl-alpha-methyl glycolate and N-benzyl-3-azabicyclo-[3.3. 1]-non-9 alpha-ol, removing benzyl on N through catalytic hydrogenation to obtain a crude product of L-demethyl benzene ring nonyl ester, salifying, and recrystallizing to obtain the L-hydrochloric acid demethyl benzene ring nonyl ester. The method is environmentally friendly and suitable for large-scale production.
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Paragraph 0067-0069
(2020/09/09)
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- Discovery of a Novel Muscarinic Receptor PET Radioligand with Rapid Kinetics in the Monkey Brain
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Positron emission tomography (PET), together with a suitable radioligand, is one of the more prominent methods for measuring changes in synaptic neurotransmitter concentrations in vivo. The radioligand of choice for such measurements on the cholinergic sy
- Malmquist, Jonas,Varn?s, Katarina,Svedberg, Marie,Vallée, Frédéric,Albert, Jeffrey S.,Finnema, Sjoerd J.,Schou, Magnus
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p. 224 - 229
(2018/03/01)
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- Stereoselective synthesis of the optical isomers of a new muscarinic receptor antagonist, HL-031120
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We present here a practical stereoselective synthetic method to produce enantiopure isomers of a new muscarinic receptor antagonist, HL-031120 (3-quinuclidinyl-2′-cyclopentyl-2′-hydroxy-2′-phenylacetate, I). Four optical isomers were effectively by stereoselective synthesized using pivaldehyde as steric hindrance agent from the chiral starting material, ( S ) or ( R )-mandelic acid. The isomers were obtained with 70-76% yields in 98-99% e.e. Copyright Taylor & Francis Group, LLC.
- Liu, Yu-Min,Liu, He,Zhong, Bo-Hua,Liu, Ke-Liang
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p. 1815 - 1822
(2007/10/03)
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- Optical resolution, stereoselective synthesis, and crystal structure of 9α-(3-azabicyclo[3,3,1]nonanyl)-2′cyclopentyl-2′-hydroxy- 2′-phenylacetate
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9α-(3-Azabicyclo[3,3,1 ]nonanyl)-2′-cyclopentyl-2′- hydroxy-2′-phenylacetate (1) was synthesized and its enantiomers were obtained by the optical resolution of racemates with the chiral host N-p-toluenesulfonylglutamic acid. Optical pure 1 was also effect
- Liu, Yan-Qing,Liu, He,Zhong, Bo-Hua,Deng, Yu-Lin,Liu, Ke-Liang
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p. 1403 - 1412
(2007/10/03)
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