- Synthesis method of (3,4-dihydro-2H-pyrano[2,3-b]pyridin-6-yl)methanol
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The invention discloses a synthesis method of a (3,4-dihydro-2H-pyrano[2,3-b]pyridin-6-yl)methanol compound. Methyl 6-hydroxy-5-iodonicotinate which is used as an initial raw material undergoes a chlorination reaction, and the obtained reaction product and tert-butyl dimethyl(prop-2-alkynyloxy)silane undergo an alkyne substitution reaction, an alkynyl reduction reaction, a TBS protection removal reaction, a cyclization reaction and reduction to obtain the target compound. The synthesis method of the (3,4-dihydro-2H-pyrano[2,3-b]pyridin-6-yl)methanol fills the blank of synthesis methods in theprior art, and the method adopting the above whole synthesis route has the advantages of good step repeatability, high conversion rate, high yield, easiness in purification, mild reaction conditions,high safety, greenness and environmental friendliness; and the obtained 4-fluoro-3-substituted-pyridine-2-formate product compound has the advantages of high purity, good quality, and facilitation ofrealization of industrialization.
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Paragraph 0080-0082
(2020/02/14)
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- Development of a safe and economical synthesis of methyl 6-chloro-5-(trifluoromethyl)nicotinate: Trifluoromethylation on kilogram scale
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Reported herein is a safe and economical synthesis of methyl 6-chloro-5-(trifluoromethyl)nicotinate, an intermediate in the synthesis of novel anti-infective agents. The key to this process is the trifluoromethylation of an aryl iodide using an inexpensive methyl chlorodifluoroacetate (MCDFA)/KF/CuI system, with an emphasis on the development work which led to this effective process.
- Mulder, Jason A.,Frutos, Rogelio P.,Patel, Nitinchandra D.,Qu, Bo,Sun, Xiufeng,Tampone, Thomas G.,Gao, Joe,Sarvestani, Max,Eriksson, Magnus C.,Haddad, Nizar,Shen, Sherry,Song, Jinhua J.,Senanayake, Chris H.
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supporting information
p. 940 - 945
(2013/07/26)
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- PROCESS FOR THE PREPARATION OF NICOTINAMIDE DERIVATIVES
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The present invention relates to a process for the preparation of nicotinamide derivatives of the formula (I) R1 to R7 are as defined in the and to pharmaceutically acceptable salts thereof. The compounds of formula (I) are useful for the treatment and / or prophylaxis of diseases which are associated with the modulation of cannabinoid 1 receptors (CB 1 receptors) as described in the PCT Publ. WO 2006/106054.
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Page/Page column 14
(2012/05/05)
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- PROCESS FOR THE PREPARATION OF NICOTINAMIDE DERIVATIVES
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The present invention relates to a process for the preparation of nicotinamide derivatives of formula I, wherein R1 to R7 are as defined above and to pharmaceutically acceptable salts thereof. The compounds of formula I are useful for the treatment and/or prophylaxis of diseases which are associated with the modulation of cannabinoid 1 receptors (CB1 receptors) as described in the PCT Publ. WO 2006/106054.
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Page/Page column 7
(2012/05/04)
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