3-甲基吡啶置于magnesium Fluoride,氢氟酸,氯体系中,化学反应 8.0H,以76.7%的收率获得产物2-氯-5-三氟甲基吡啶 参考文献:Method For Preparing 2,3-Dichloro-5-Trifluoromethylpyridine With High Selectivity 标题:Method For Preparing 2,3-Dichloro-5-Trifluoromethylpyridine With High Selectivity 摘要:本发明公开了一种制备2,3-二氯-5-三氟甲基吡啶的方法,包括在100~150oc温度和0.5~5.0 Mp压力下,在至少选择自支持金属氯化物,支持沸石分子筛和支持杂多酸的催化剂存在下,2-氯-5-三氟甲基吡啶与氯气反应得到2,3-二氯-5-三氟甲基吡啶.本发明提供的制备方法具有所需产品高选择性,氯气利用率高,工艺条件适中,操作简单和三废少等优点.本发明还公开了一种制备2-氯-5-三氟甲基吡啶的制备方法,与现有技术相比,能够降低单位消耗,减少分离成本,并提高安全性.
专利号:WO-2022099693-A1 优先权日:2020-11-16 标题 :Method for improving effect of fluorination reaction in synthesis of 2-chloro-5-trifluoromethyl pyridine, and matching system 发明人:ZHA ZHIXIONG; LI HAO 权利人:SHANXIAN XINRUN CHEMICAL CO LTD 摘要:The present invention relates to the technical field of chemical synthesis, and particularly, a method for improving effect of fluorination reaction in the synthesis of 2-chloro-5-trifluoromethyl pyridine, and a matching system. The method comprises the following steps: preparing 2-chloro-5-trichloromethyl pyridine, and adding to an efficient reaction system after superfine crushing; adding an appropriate amount of iodine pentafluoride, mercury fluoride and a catalyst into the efficient reaction system; controlling the temperature and time, and carrying out a fluorination reaction on materials in the high-pressure, sealed, efficient reaction system to obtain a crude solution containing 2-chloro-5-trifluoromethyl pyridine; purifying the above crude solution to obtain 2-chloro-5-trifluoromethyl pyridine. In the present method, a fluorination reaction is carried out in a high-pressure sealed environment, such that the efficiency and effect of the fluorination reaction are effectively improved. By means of the system in the present invention, the material entering the system may be quickly superfine crushed before the reaction, so as to improve the reaction sufficiency in the subsequent reaction process.
专利号:EP-0058173-B1 优先权日:1980-08-26 标 题:Process for the synthesis of aryloxy derivatives 摘要:Process for the synthesis of compounds of formula I (FORMULA) wherein O, is a substituted or unsubstituted aryl or heteroaryl group and U and V may be chosen from a range of substituents including hydrogen, halogen, alkyl and alkoxy; the process comprising reacting a sulfate ester of formula II, wherein Q is a cation, with a compound of formula III, wherein L is a leaving group (FORMULA) and hydrolysing the sulfate ester formed. Preferably the sulfate ester of formula II is prepared by the oxidation of a phenol of formula IV with a persulfate.
专利号:US-2008300251-A1 优先权日:2005-09-05 标 题 :Derivatives of 3-Azabicyclo[3.1.0] Hexane as Dipeptidyl Peptidase-IV Inhibitors 发明人:SATTIGERI JITENDRA A; ANDAPPAN MURUGAIAH M S; KISHORE KAUSHAL; SETHI SACHIN; KANDALKAR SACHIN RAMESH; PAL CHANCHAL KUMAR; MAHAJAN DIPAK C; AHMED SHAHADAT; PARKALE SANTHOSH SADASHIV; SRINIVASAN T; SHARMA LALIMA; BANSAL VINAY S; CHUGH ANITA; DAVIS JOSEPH ALEXANAND 权利人:SATTIGERI JITENDRA A; ANDAPPAN MURUGAIAH M S; KISHORE KAUSHAL; SETHI SACHIN; KANDALKAR SACHIN RAMESH; PAL CHANCHAL KUMAR; MAHAJAN DIPAK C; AHMED SHAHADAT; PARKALE SANTHOSH SADASHIV; SRINIVASAN T; SHARMA LALIMA; BANSAL VINAY S; CHUGH ANITA; DAVIS JOSEPH ALEXANAND 摘要:The present invention relates to novel 3-azabicyclo[3.1.0]hexane derivatives as dipeptidyl peptidase-IV inhibitors and the processes for the synthesis of the said compounds. This invention also relates to pharmacological compositions containing the compounds of the present invention, and methods of treating diabetes, especially type 2 diabetes, as well as prediabetes, diabetic dyslipidemia, metabolic acidosis, ketosis, satiety disorders, and obesity. These inhibitors can also be used to treat conditions manifested by a variety of metabolic, neurological, anti-inflammatory, and autoimmune disorders like inflammatory disease, multiple sclerosis, rheumatoid arthritis; viral, cancer and gastrointestinal disorders. The compounds of this invention can also be used for treatment of infertility arising due to polycystic ovary syndrome.
专利号:WO-2022099691-A1 优先权日:2020-11-16 标 题 :Device and production method for continuously generating 2-chloro-5-trifluoromethylpyridine 发明人:LI HAO 权利人:SHANXIAN XINRUN CHEMICAL CO LTD 摘要:The present invention relates to a device for continuously generating 2-chloro-5-trifluoromethylpyridine. Further disclosed is a production method for continuously generating 2-chloro-5-trifluoromethylpyridine, benzyl chloride is used as a raw material, and the product is obtained by passing through amination, condensation, acetylation, cyclization, and then chlorination and fluorination, and the method specifically comprises the following steps: S1, synthesis of benzylamine; S2, synthesis of N-benzyl-N-(propenyl)-acetamide; S3, synthesis of 2-chloro-5-methylpyridine; S4, synthesis of 2-chloro-5-trifluoromethylpyridine; and S5, refining of 2-chloro-5-trifluoromethylpyridine. The present invention has the following beneficial effects: in the device and production method for continuously generating 2-chloro-5-trifluoromethylpyridine of the present invention, the synthesis process route of the present invention is simple and efficient, the cost of raw materials is low, the purity of the obtained product is high, production safety is ensured, and industrialization and promotion are easy.
专利号:WO-2022099692-A1 优先权日:2020-11-16 标题 :Method and system for synthesizing 2-chloro-5-trifluoromethyl pyridine 发明人:ZHA ZHIXIONG; GUO YONGLI 权利人:SHANXIAN XINRUN CHEMICAL CO LTD 摘要:The present invention relates to the technical field of chemical synthesis, and particularly, to a method and system for synthesizing 2-chloro-5-trifluoromethyl pyridine. The method comprises the following steps: S1: preparing raw materials; S2: carrying out a chlorination reaction; S3: adding an initiator and sufficient catalyst to a 2-chloro-5-methylpyridine product obtained from the above steps, and controlling an initiation reaction to obtain a crude 2-chloro-5-trichloromethyl pyridine; S4: distilling and purifying the product from above steps to obtain a refined 2-chloro-5-trichloromethyl pyridine; S5: separating and purifying, for the second time, the 2-chloro-5-trichloromethyl pyridine to be used; S6: carrying out a fluorination reaction; S7: transferring the crude solution to a downstream process of a product synthesis system for purification, and obtaining a refined 2-chloro-5-trifluoromethyl pyridine. The present method uses a combination of a chlorination reaction and a fluorination reaction in the synthesis of 2-chloro-5-trifluoromethyl pyridine to obtain the product, and also ensures product yield and quality by means of efficient purification.
专利号:US-7754188-B2 优先权日:2003-06-30 标 题:Radiolabeled cannabinoid-1 receptor modulators 发明人:BURNS H DONALD; CHEN ALEX M; GIBSON RAYMOND E; GOULET MARK T; HAGMANN WILLIAM K; HAMILL TERENCE G; JEWELL JAMES P; LIN LINUS S; LIU PING; PERESYPKIN ANDREY V 权利人:MERCK SHARP & DOHME 摘要:The present invention relates to particular radiolabeled Cannabinoid-1 (CB1) receptor modulators, and methods of using these modulators for labeling and diagnostic imaging of Cannabinoid-1 receptors in mammals, particularly humans. In addition, intermediates useful for the synthesis of the radiolabeled Cannabinoid-1 receptor modulators are also disclosed, as well as the processes for synthesizing the radiolabeled Cannabinoid-1 receptor modulators. Still further, formulations of the radiolabeled Cannabinoid-1 receptor compounds are described.