1260893-58-0

Upstream product

• 1034025-91-6 1,3-diethyl (2,5-difluoro-4-nitrophenyl)propanedioate 
• 2105-61-5 1,2,4-trifluoro-5-nitrobenzene 
• 770719-22-7 (2,5-difluoro-4-nitrophenyl)acetic acid 
• 1034025-94-9 1,3-diethyl 2-(4-amino-2,5-difluorophenyl)propanedioate 

Downstream Products

• 1374573-64-4 [2,5-difluoro-4-(1H-tetrazol-1-yl)phenyl]acetic acid 
• 209995-38-0 (2,4,5-trifluorophenyl)acetic acid 

Relevant academic research and scientific papers

A 2, 4, 5-trifluorophenylacetic acid method for the preparation of

The invention discloses a preparation method 2,4,5-trifluorophenylacetic acid. The method is characterized by consisting of four reaction steps of: A, reaction of 2,4,5-trifluoronitrobenzene (I) and diethyl malonate which are condensed to prepare 2,5-difloro-4-nitrobenzophenone diethyl malonate; B, hydrolysis, acidification and decarboxylic reaction of dibasic ester; C, reduction reaction of nitryl; and D, diazotization fluoridation of amino. The four reaction steps can be sequentially carried out according to A, B, C and D, or A, C, B and D, or A, C, D and B. According to the preparation method provided by the invention, condensation of 2,4,5-trifluoronitrobenzene (I) and diethyl malonate is easy to realize by means of high substituting activity of nitryl p-fluorine, and the raw material 2,4,5-trifluoronitrobenzene (I) is low in cost and easy to obtain and can be easily prepared by nitration and fluorination of 2,4-dichlor fluorbenzene. Compared with the prior art, the preparation method provided by the invention has the characteristics of low-cost and easily obtained raw materials, mild reaction condition, high total yield, low production cost and the like, and is comparatively suitable for industrialized production.

INHIBITORS OF RENAL OUTER MEDULLARY POTASSIUM CHANNEL

Novel spirocyclic compounds of formula I: and pharmaceutically acceptable salts thereof are disclosed as inhibitors of the ROMK (Kir1.1) channel. The compounds may be used as diuretic and/or natriuretic agents and for the therapy and prophylaxis of medical conditions including cardiovascular diseases such as hypertension, heart failure and chronic kidney disease and conditions associated with excessive salt and water retention. Pharmaceutical compositions and methods of treatment are also included.

INHIBITORS OF THE RENAL OUTER MEDULLARY POTASSIUM CHANNEL

Novel spirocyclic compounds of formula I: and pharmaceutically acceptable salts thereof are disclosed as inhibitors of the ROMK (Kir1.1) channel. The compounds may be used as diuretic and/or natriuretic agents and for the therapy and prophylaxis of medical conditions including cardiovascular diseases such as hypertension, heart failure and chronic kidney disease and conditions associated with excessive salt and water retention. Pharmaceutical compositions and methods of treatment are also included.

INHIBITORS OF THE RENAL OUTER MEDULLARY POTASSIUM CHANNEL

The present invention provides compounds of Formula I and the pharmaceutically acceptable salts thereof, which are inhibitors of the ROMK (Kirl.1) channel. The compounds may be used as diuretic and/or natriuretic agents and for the therapy and prophylaxis of medical conditions including cardiovascular diseases such as hypertension, heart failure and conditions associated with excessive salt and water retention.