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Synthesis of phosphodiesterase 9A inhibitor LW33
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Ri-bin QIAN1, Jian-song WANG2, Hai-hong YE1, Ying-xia BAO1
Chinese Journal of New Drugs | 2021, 30(2) : 114 - 118
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Chinese Journal of New Drugs | 2021, 30(2): 114-118
Synthesis of phosphodiesterase 9A inhibitor LW33
Full
Ri-bin QIAN1, Jian-song WANG2, Hai-hong YE1, Ying-xia BAO1
Affiliations
  • 1Guangzhou Baiyunshan Pharmaceutical Co., Ltd., Guangzhou Baiyunshan Pharmaceutical General Factory, Guangzhou 510515, China
  • 2Guangzhou Baiyunshan Pharmaceutical Co., Ltd., Guangzhou 510130, China
Published: 2021-01-30
Outline
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Objective:

To optimize the synthesis process of LW33.

Methods:

Using 2,4,6-trichloro-5-pyrimidine-carboxaldehyde and aminomethylcyclopentane hydrochloride as starting materials, (S)-6-[(1-(4-chlorophenyl)ethyl)amino]-1-cyclopentyl-1,5,6,7-tetrahydro-4H-pyrazolo [3,4-d] pyrimidin-4-one, a novel phosphodiesterase 9A (PDE 9A) inhibitor, LW33 was synthesized through three steps.

Results:

The structure of LW33 was verified by 1H-NMR, 13C-NMR and ESI-HRMS. The verified target material LW33 was synthesized with a total yield of 43.6%, and the purity was 99.9% as determined by HPLC.

Conclusion:

With high purity and yield, the improved process is easy to operate in a mild condition. It is suitable for further industrial production.

phosphodiesterase 9A inhibitor  /  LW33  /  synthesis
钱日彬, 王健松, 叶海鸿, 鲍颖霞. 磷酸二酯酶9A抑制剂LW33的合成. 中国新药杂志, 2021 , 30 (2) : 114 -118 .
Ri-bin QIAN, Jian-song WANG, Hai-hong YE, Ying-xia BAO. Synthesis of phosphodiesterase 9A inhibitor LW33[J]. Chinese Journal of New Drugs, 2021 , 30 (2) : 114 -118 .
Year 2021 volume 30 Issue 2
24
5
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  • Online Date:2026-10-29
  • Published:2021-01-30
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  • Accepted:2020-04-07
Funding
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    1Guangzhou Baiyunshan Pharmaceutical Co., Ltd., Guangzhou Baiyunshan Pharmaceutical General Factory, Guangzhou 510515, China
    2Guangzhou Baiyunshan Pharmaceutical Co., Ltd., Guangzhou 510130, China
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表12种不同金属材料的力学参数
科
Family
属数
Number of
genus
种数
Number of
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Genus
种数
Number of
species
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Percentage of total
species (%)
鹅膏菌科Amanitaceae 2 11 5.26 鹅膏菌属 Amanita 10 4.78
小菇科 Mycenaceae 2 12 5.74 丝盖伞属 Inocybe 5 2.39
多孔菌科 Polyporaceae 8 14 6.70 蜡蘑属 Laccaria 5 2.39
红菇科 Russulaceae 3 23 11.00 小皮伞属 Marasmius 6 2.87
小菇属 Mycena 11 5.26
光柄菇属 Pluteus 5 2.39
红菇属 Russula 17 8.13
栓菌属 Trametes 5 2.39
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