期刊
ORGANIC PROCESS RESEARCH & DEVELOPMENT
卷 19, 期 7, 页码 831-840出版社
AMER CHEMICAL SOC
DOI: 10.1021/acs.oprd.5b00101
关键词
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资金
- University of Nottingham EPSRC Impact Acceleration Account [EP/K503800/1]
- EPSRC [EP/G026882/1] Funding Source: UKRI
- Engineering and Physical Sciences Research Council [EP/K50354X/1, EP/K503800/1, EP/G026882/1] Funding Source: researchfish
Methods for the batch scale up of DABAL-Me-3 promoted direct ester to amide synthesis have been demonstrated at 10-100 g scales using a tert-amide model compound. Procedures for 20 g scale couplings in standard laboratory glassware and up to 0.1 kg in industry-standard jacketed glass reactors in near quantitative yields are given. A derivative of the anticancer agent Imatinib (Gleevec) has been synthesized on a 26 g scale (98% yield, >98% purity) establishing DABAL-Me-3 as a potential alternative for the synthesis of amides in API scale preparations. Continuous flow methodology provides a method for larger scales (productivities of >50 g h(-1)). In addition, nitriles were coupled to primary amines and hydrazines with DABAL-Me-3, resulting in the clean formation of free amidines (16 examples) and amidrazones.
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