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Efficient Azacycle Formations Developed in Japanese Pharmaceutical Industries: Elegancy, Logistics, and Training (ELT) "Sandwich" for Process Chemists
被引：0
|作者：
Mizufune, Hideya
[1
]
机构：
[1] SPERA PHARMA Inc, Chem R&D Div, Yodogawa Ku, 17-85 Jusohonmachi 2 Chome, Osaka 5320024, Japan
关键词：
nitrogen-containing heterocycles;
azacycles;
process chemistry;
raw materials;
molecular diversity;
LARGE-SCALE SYNTHESIS;
PALLADIUM-CATALYZED BENZANNULATION;
PRACTICAL SYNTHESIS;
SCALABLE SYNTHESIS;
REGIOSELECTIVE SYNTHESIS;
KINASE INHIBITOR;
DERIVATIVES;
DRUG;
CYCLIZATION;
ANTAGONIST;
D O I：
10.1021/acs.oprd.8b00412
中图分类号：
O69 [应用化学];
学科分类号：
081704 ;
摘要：
Efficient azacycle (nitrogen-containing heterocycle) formations developed by chemists in Japanese pharmaceutical industries have been selected from the published articles since the year 2000. The selected examples have been classified by the nitrogen source in the raw materials and have been reviewed from the following process chemistry perspectives; elegancy to establish the active pharmaceutical ingredient synthetic processes, logistics to procure/transform the required raw materials, and training for process chemists to consider azacycle formations according to a systematic approach. This mini-review also focuses on the molecular diversity created by the azacycle formations.
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页码：419 / 442
页数：24
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