Boc-(R)-3-Amino-4-(2,4,5-trifluorophenyl)butanoic acid

CAS NO.：486460-00-8
Empirical Formula: C15H18F3NO4
Molecular Weight: 333.3
MDL number: MFCD06659147
EINECS: 691-120-8
SAFETY DATA SHEET (SDS)
Update Date: 2026-05-28 04:57:51

What is Boc-(R)-3-Amino-4-(2,4,5-trifluorophenyl)butanoic acid?

Description

Boc-(R) -3-amino-4 -(2,4, 5-trifluorophenyl) butyric acid is an important intermediate for the preparation of sitagliptin. Sitagliptinphosphate is the first dipeptidase -IV(dpp-4) inhibitor approved by FDA in 2006. It is used for the treatment of type II diabetes mellitus. It has obvious hypoglycemic effect when used alone or in combination with metformin and pioglitazone, and it is safe to take, well tolerated, with few adverse reactions.

The Uses of Boc-(R)-3-Amino-4-(2,4,5-trifluorophenyl)butanoic acid

(R)-3-((tert-Butoxycarbonyl)amino)-4-(2,4,5-trifluorophenyl)butanoic Acid has been used as a reactant for the preparation of dipeptidyl peptidase-4 (DPP4) inhibitors for the treatment of type 2 diabetes, such as sitagliptin.

Synthesis

(R)-β-tert-butoxycarbonylamino-2,4,5-trifluorophenylbutyric acid ethyl ester could used as a starting material and followed by adding Methanol and LiOHH2O as reaction reagents. Adding dichloromethane to the concentrate and adjust the pH to 2 with 2N HCl. Boc-(R)-3-Amino-4-(2,4,5-trifluorophenyl)butanoic acid could be obtained through further purification.

Properties of Boc-(R)-3-Amino-4-(2,4,5-trifluorophenyl)butanoic acid

Melting point:	136-138℃
Boiling point:	443.1±45.0 °C(Predicted)
Density	1.292±0.06 g/cm3(Predicted)
storage temp.	2-8°C
solubility	Chloroform (Slightly), DMSO (Slightly), Ethyl Acetate (Slightly), Methanol (Slig
form	Solid
pka	4.30±0.10(Predicted)
color	White to Off-White

Safety information for Boc-(R)-3-Amino-4-(2,4,5-trifluorophenyl)butanoic acid

Signal word	Warning
Pictogram(s)	Exclamation Mark Irritant GHS07
GHS Hazard Statements	H319:Serious eye damage/eye irritation
Precautionary Statement Codes	P305+P351+P338:IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.