790712-60-6

Usage

Uses

Used in Food and Beverage Industry:
Phosphoric acid is used as a flavoring and preservative agent for its ability to provide a tangy taste and extend the shelf life of carbonated soft drinks and other food products.
Used in Fertilizer Production:
Phosphoric acid is utilized as a key ingredient in the manufacture of fertilizers, contributing to the production of essential nutrients for plant growth.
Used in Detergent and Pharmaceutical Industries:
It serves as a crucial component in the production of detergents and pharmaceuticals, enhancing their effectiveness and performance.
Used in Metal Treatment and Cleaning Products:
Phosphoric acid is employed in the production of metal treatment and cleaning products, where its strong acidic properties aid in the removal of impurities and rust.
Caution:
Due to its highly corrosive nature, phosphoric acid should be handled with care to avoid skin and eye irritation, as well as burns. Proper safety measures and precautions must be taken during its use.

Upstream product

• 86119-84-8 phosphoric acid 
• 486460-32-6 sitagliptin 
• 823817-56-7 (R/S)-4-oxo-4-[3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-1-(2,4,5-trifluorophenyl)butan-2-amine 
• 1240038-86-1 sitagliptin (R)-(-)mandelate 
• 327-52-6 1-bromo-2,4,5-trifluorobenzene 
• 1293293-73-8 (3R)-3-azido-4-(2,4,5-trifluorophenyl)-butyric acid 
• 1246960-15-5 (S)-1-chloro-3-(2,4,5-trifluorophenyl)propan-2-ol 
• 1283096-72-9 (2S)-2-(2,4,5-trifluorobenzyl)-oxirane 
• 1293293-72-7 (2S)-1-(2-azido-4-pentenyl)-2,4,5-trifluorobenzene 
• 1293293-71-6 (2R)-1-(2,4,5-trifluorophenyl)-4-pentene-2-ol 
• 1329036-41-0 C₁₂H₁₃F₃O₃S 
• 1329036-44-3 (3R)-3-azido-(2,4,5-trifluorophenyl)butyric acid (R)-methylbenzylamine salt 
• 1329036-54-5 C₁₀H₇ClF₃N₃O 
• 1380521-84-5 tert-butyl (E)-4-(2',4',5'-trifluorophenyl)but-2-enoate 

Relevant academic research and scientific papers

IMPROVED PROCESS FOR PREPARATION OF SITAGLIPTIN

Provided herein is a process for the preparation of specific enantiomeric Sitagliptin with good chiral purity and higher yield using improved biocatalyst and by engineering an enzyme to mediate the efficient conversion of ketoamide to obtain enantiomerically pure Sitagliptin in presence of an amino group donor.

Synthesis of (?)-(R)-Sitagliptin by RhI-Catalyzed Asymmetric Hydroamination

We report of a concise synthesis of (R)-sitagliptin monophosphate – a drug predominantly applied in the treatment of type 2 diabetes. Utilizing our recently developed RhI-catalyzed hydroamination of allenes for the stereoselective construction of the inherent chiral amino function, a new approach to (R)-sitagliptin monophosphate on a 3.5 mmol scale was established.

Two methods for the preparation of sitagliptin phosphate: Via chemical resolution and asymmetric hydrogenation

Two effective processes have been developed for the preparation of sitagliptin phosphate. The approach of chemical resolution obtained R-sitagliptin in five steps from commercially available starting materials using the inexpensive NaBH4 to reduce the enamine and then using (-)-di-p-toluoyl-l-tartaric acid to resolve racemates in 11% yield overall. The route successfully avoids the use of expensive noble metal as catalysts compared with traditional synthesis methods, resulting in greatly reduced costs and simplified synthetic routes. Other alternative asymmetric hydrogenation of β-ketomide routes for the synthesis of sitagliptin were found, two of the intermediates were synthesized for the first time. This journal is

Process for preparing sitagliptin

The present technology relates to a method for manufacturing sitagliptin, which is a representative drug among DPP-4 inhibitors which are drugs used for the treatment of diabetes. The method of the present invention uses CDI for the condensation reaction of specific compounds, and through a specific subsequent process, high-purity sitagliptin phosphate monohydrate can be manufactured in a high yield. In particular, the manufacturing method of the present invention is suitable for mass production.

Preparation method of sitagliptin phosphate monohydrate crystal form

The invention relates to a preparation method of a sitagliptin phosphate monohydrate crystal form. The method comprises the following steps: adding sitagliptin free alkali, phosphoric acid, water and a specific organic solvent into a reactor, and reacting

Synthesis of (R)-3-(tert-Butoxycarbonylamino)-4-(2,4,5-trifluorophenyl)butanoic Acid, a Key Intermediate, and the Formal Synthesis of Sitagliptin Phosphate

An alternate formal synthesis of Sitagliptin phosphate is disclosed from 2,4,5-trifluorobenzadehyde in 8 linear steps with an overall yield of 31%. The chiral β-amino acid moiety present in sitaglitpin is installed via an asymmetric hydrogenation followed by a stereoselective Hofmann rearrangement as the key steps. The key chiral intermediate Boc-amino acid 1 prepared by this novel route was further converted to Sitagliptin phosphate following the known literature protocol.

Preparation method of sitagliptin phosphate

The invention discloses a preparation method of sitagliptin phosphate. The preparation method comprises the following steps: taking 4-(2, 4, 5-trifluorophenyl)-3-methyl oxobutyrate I as a raw material; the reaction is mainly divided into five steps: carrying out asymmetric reduction on the raw material I through an N-heterocyclic carbene palladium catalyst to obtain chiral alcohol ester s-4-(2, 4,5-trifluorophenyl)-3-methyl hydroxybutyrate II; carrying out intramolecular condensation cyclization on the II to obtain chiral lactam quaternary ring (R)-N-benzyloxy-4-[1-methyl-(2, 4, 5-trifluorophenyl)]-2-azetidinone III; carrying out ring opening on the III under an alkaline condition to obtain IV; performing condensation reaction to form amide to obtain V; carrying out catalytic reduction onthe V through recycled N-heterocyclic carbene palladium to remove benzyloxy and form phosphate to obtain sitagliptin phosphate VI, wherein the N-heterocyclic carbene palladium catalyst is Pd (IPr-NHC) (acac) Cl or Pd (IPr-NHC) (acac) Oac or Pd (IPr-NHC) (dba) Cl or Pd (IPr-NHC) (dba) OAc; the catalyst is cheap and easily available, can be recycled, and is beneficial to batch production.

PROCESSES FOR THE PREPARATION OF SITAGLIPTIN AND PHARMACEUTICALLY ACCEPTABLE SALTS THEREOF

The present application relates to improved processes for the preparation of Sitagliptin and pharmaceutically acceptable salts thereof. The present application also relates to the improved crystallization process for the preparation of Sitagliptin Phosphate. The present application also relates to the improved crystallization process for the preparation of Sitagliptin Hydrochloride monohydrate.

Preparation method of sitagliptin phosphate anhydrous hydrate

The invention relates to a preparation method, of a crystal form of sitagliptin phosphate anhydrous crystal, which is used for preparing sitagliptin phosphate anhydrous crystal form, with high yield, purity, particles after heating the solution, filtering

Preparation method of Sitagliptin phosphate monohydrate crystal form

The invention relates to a preparation method of a Sitagliptin phosphate monohydrate crystal form, and the method specifically comprises the following steps: taking water as a solvent, heating, dissolving, cooling, carrying out suction filtration, and dry