72537-17-8Relevant articles and documents
Preparation method of 2-fluorine-3-chlorine-5-trifluoromethylpyridine
-
Paragraph 0026; 0027; 0028; 0033; 0036, (2018/07/30)
The invention relates to the technical field of chemical synthesis, and in particular discloses a preparation method of 2-fluorine-3-chlorine-5-trifluoromethylpyridine. The preparation method of the 2-fluorine-3-chlorine-5-trifluoromethylpyridine is characterized by comprising the following steps: taking 2-chlorine-5-trichloromethylpyridine as a raw material, taking tungsten hexachloride as a catalyst, heating and introducing chlorine to perform chlorination reaction, thereby obtaining 2,3-dichloro-5-trichloromethylpyridine; putting the 2,3-dichloro-5-trichloromethylpyridine into a fluorination kettle, adding antimony pentafluoride and anhydrous hydrogen fluoride, stirring and heating to perform reaction, cooling after reaction, washing with water, layering, feeding to a rectification kettle, and performing reduced-pressure rectification, thereby preparing the 2-fluorine-3-chlorine-5-trifluoromethylpyridine. The process is reliable, the raw materials are sufficient in the market and easily available, and the preparation method of the 2-fluorine-3-chlorine-5-trifluoromethylpyridine is low in production cost, simple in operation, high in yield and favorable for large-scale production.
Bitopertin synthetic method and intermediate
-
Paragraph 0061-0063, (2018/03/26)
The present invention discloses a new synthesis method and intermediates of Bitopertin. According to the Bitopertin synthesis method, 5-methylsulfonyl-2-[(1S)-2,2,2-trifluoro-1-methylethoxy]benzoic acid is adopted as a raw material, and continuous multi-step operations such as chlorination, acylation, deprotection, condensation and re-crystallization are subjected to performed to obtain the Bitopertin, wherein the intermediates in each step do not require further purification, and the total yield can achieve more than or equal to 80%.
A 2 - cyano - 3 - chloro - 5 - trifluoro methyl pyridine synthesis method (by machine translation)
-
Paragraph 0032; 0033, (2017/11/04)
The invention discloses a 2 - cyano - 3 - chloro - 5 - trifluoro methyl pyridine synthesis method, which belongs to the technical field of organic synthesis. The method includes the steps of: (1) to 2, 3 - dichloro - 5 - trifluoro methyl pyridine as raw material, in the solvent system is added in the catalyst, by fluorination synthesis of 2 - fluoro - 3 - chloro - 5 - trifluoro methyl pyridine, (2) in the step 1 of the 2 - fluoro - 3 - chloro - 5 - trifluoro methyl pyrrole cyanide reagent carbonitriding after adding, after the water washing, after the distillation, shall be 2 - cyano - 3 - chloro - 5 - trifluoro methyl pyridine. The purity of the product can reach 99.5%, the yield can be 90%, the reaction condition during the mild, easy to operate, and is suitable for large-scale production. (by machine translation)
3 - chloro -5 - trifluoromethyl pyridine compounds and intermediates method (by machine translation)
-
Paragraph 0077; 0078; 0079; 0080; 0081; 0082; 0083-0085, (2017/07/20)
The invention discloses a 3 - chloro -5 - trifluoromethyl pyridine compound and preparation method of the midbody. The invention of the formula 3 a compound represented by the preparation method, comprising the following steps: organic solvent and water in the mixed solvent, under the action of the phase transfer catalyst, shown as 2 shown with the metal cyanide compounds of the substitution reaction, carbonized 3 compound of formula; further comprises the following steps: in the solvent, under the effect of the fluorination reagent, shown as 1 shown in the fluorination reaction of the compound, prepared states like the type 2 compound of formula; and can also be further comprises the following steps: under the action of the hydrogen and ethanol, shown as 3 shown in the Pinner reaction compound, then hydrolyzing the ester reaction, carbonized 4 compounds are shown. The invention of 3 - chloro -5 - trifluoromethyl pyridine compound preparation method of low cost, high production safety, simple operation, high yield, it is suitable for industrial production. (by machine translation)
SYNTHESIS OF GLYT-1 INHIBITORS
-
Page/Page column 9-10, (2008/12/08)
The present invention relates to a process for preparation of a compound of formula I wherein Het, R1, R2, R3, and n are as defined herein and pharmaceutically acceptable acid addition salts thereof, which comprises reacting a compound of formula 21 with a compound of formula 8 to obtain a compound of formula 11 and coupling the compound of formula 11 in the presence of a coupling reagent or the corresponding acid halogenide with a compound of formula 15 to obtain a compound of formula I.
Process for the preparation of 2-aminomethylpyridines
-
Page 6, (2008/06/13)
The invention relates to a process for the preparation of a compound of formula (I): wherein X, Y and n are as defined in the description.
Facile preparation of aromatic fluorides by deaminative fluorination of aminoarenes using hydrogen fluoride combined with bases
Yoneda,Fukuhara
, p. 23 - 36 (2007/10/02)
One-pot deaminative fluorination of aminoarenes including heteroaromatics, namely, diazotization of aminoarenes followed by in situ fluoro-dediazoniation of the corresponding diazonium ions, was successfully accomplished to produce fluoroarenes in high yields by using hydrogen fluoride combined with base solutions. The diazotization stage has been found to play the most important part in yielding fluoroarenes effectively. It was greatly influenced by the composition of the HF solution and enhanced by employing appropriate amounts of bases such as pyridine under carefully controlled conditions. The fluoro-dediazoniation stage was effectively accelerated photochemically to afford fluoroarenes having polar substituents such as hydroxyl, nitro and so on in high yields.
A Facile Preparation of Fluoropyridines from Aminopyridines via Diazotation and Fluorodediazoniation in HF or HF-Pyridine Solutions
Fukuhara, Tsuyoshi,Yoneda, Norihiko,Suzuki, Akira
, p. 435 - 438 (2007/10/02)
Fluoropyridines were prepared in high yields by dizotation of aminopyridines in HF or HF-pyridine solutions, followed by dediazoniation in situ at 20-60 deg C.
