13091-23-1Relevant articles and documents
CHLORINE-ISOTOPIC EXCHANGE BETWEEN LITHIUM CHLORIDE AND SUBSTITUTED 2-CHLOROPYRIDINE IN HOMOGENEOUS SOLUTION
Gore, Peter H.,Hundal, Apparapar S.,Morris, Donald F. C.
, p. 167 - 171 (1981)
The kinetics of chlorine-isotopic exchange between lithium chloride-36 and cyano- and nitro-substituted 2-chloropyridines were measured in sulpholane, acetone or methanol solution.Activating effects of ortho-nitro and ortho-azu substitution are compared: a nitro-group is 50 x as activating as the aza-group in the p-nitrochlorobenzene system, whereas it is the aza-function which is 3 times as activiting as the nitro group in the o-nitrochlorobenzene system.The effect of Me substituents placed ortho to an activating nitro-group was studied by comparing 2-chloro-3-cyano-5-nitropyridine and its 6-methyl- and 4,6-dimethyl derivatives.
Synthetic method of active intermediate 4-chloro-3-nitropyridine
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Paragraph 0013; 0019; 0025, (2021/04/28)
The invention discloses a synthetic method of active intermediate 4-chloro-3-nitropyridine. The method comprises the following steps: step 1, adding 24L of concentrated sulfuric acid into a 50L reaction kettle, cooling to about 10 DEG C, adding 4kg of raw materials in batches, carrying out HPLC detection on the end of the reaction of the raw materials on the next day, carrying out aftertreatment, slowly pouring the reaction liquid into 30L of ice water for quenching, adjusting the pH value to 7, carrying out suction filtration to obtain a faint yellow solid, and carrying out suction filtration; drying to obtain 4.6 kg of 4-hydroxy-3-nitropyridine faint yellow solid with the yield of 80% and the purity of 98%; and 2, adding 500g of SM into a 10L reaction flask at room temperature, dissolving with 5L of methylbenzene, dropwise adding 1643g of phosphorus oxychloride at room temperature, dropwise adding the crude product into PE, stirring and extracting for multiple times to obtain 388g of 4-chloro-3-nitropyridine faint yellow solid with the yield of 68% and the purity of 95%. According to the synthetic method of active intermediate 4-chloro-3-nitropyridine, improvement points of the project process mainly aim at purity control and reaction stability control of the reaction in the third step, aftertreatment is simple, and product purification can be achieved through extraction.
NOVEL AROMATIC COMPOUND AND USE THEREOF
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Paragraph 0330-0332, (2016/08/17)
Provided is a compound showing a bone formation promoting action (and/or bone resorption suppressive action). A compound of the formula (I) or a pharmacologically acceptable salt: [wherein each substituent is as defined in the DESCRIPTION], has low toxicity, shows good pharmacokinetics, has an action to promote bone formation, and is useful for the prophylaxis or To treatment of metabolic bone diseases (osteoporosis, fibrous osteitis (hyperparathyroidism), osteomalacia, Paget's disease that influences the systemic bone metabolism parameter etc.) associated with a decrease in the bone formation ability as compared to the bone resorption capacity.
