Anagliptin
- Product Name
- Anagliptin
- CAS No.
- 739366-20-2
- Chemical Name
- Anagliptin
- Synonyms
- Suiny;SK-0403;Anagliptin;SUINY;SK-0403;Anagliptin API;Anagliptin (SK-0403);(S)-N-(2-(2-(2-cyanopyrrolidin-1-yl)-2-oxoethylaMino)-2-Methylpropyl)-2-Methylpyrazolo[1,5-a]pyriMidine-6-carboxaMide;(R)-N-(2-(2-(2-cyanopyrrolidin-1-yl)-2-oxoethylamino)-2-methylpropyl)-2-methylpyrazolo[1,5-a]pyrimidine-6-carboxamide;N-[2-[[2-[(2S)-2-Cyano-1-pyrrolidinyl]-2-oxoethyl]amino]-2-methylpropyl]-2-methylpyrazolo[1,5-a]pyrimidine-6-carboxamide;N-[2-[[2-[(2S)-2-cyanopyrrolidin-1-yl]-2-oxoethyl]amino]-2-methylpropyl]-2-methylpyrazolo[1,5-a]pyrimidine-6-carboxamide
- CBNumber
- CB52627327
- Molecular Formula
- C19H25N7O2
- Formula Weight
- 383.45
- MOL File
- 739366-20-2.mol
Anagliptin Property
- Melting point:
- 115 - 119°C
- Density
- 1.33±0.1 g/cm3(Predicted)
- storage temp.
- Refrigerator
- solubility
- Chloroform (Slightly), Dichloromethane (Slightly), DMSO (Slightly)
- form
- Solid
- pka
- 12.40±0.46(Predicted)
- color
- White to Off-White
Hazard and Precautionary Statements (GHS)
- Symbol(GHS)
-
- Signal word
- Warning
- Hazard statements
-
H302Harmful if swallowed
- Precautionary statements
-
P280Wear protective gloves/protective clothing/eye protection/face protection.
P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.
N-Bromosuccinimide Price
- Product number
- A637210
- Product name
- Anagliptin
- Packaging
- 1mg
- Price
- $80
- Updated
- 2021/12/16
- Product number
- FA31542
- Product name
- Anagliptin
- Packaging
- 2mg
- Price
- $100
- Updated
- 2021/12/16
- Product number
- FA31542
- Product name
- Anagliptin
- Packaging
- 5mg
- Price
- $200
- Updated
- 2021/12/16
- Product number
- CS-4510
- Product name
- Anagliptin
- Purity
- ≥97.0%
- Packaging
- 10mg
- Price
- $240
- Updated
- 2021/12/16
- Product number
- FA31542
- Product name
- Anagliptin
- Packaging
- 10mg
- Price
- $350
- Updated
- 2021/12/16
Anagliptin Chemical Properties,Usage,Production
Description
Anagliptin is a dipeptidyl peptidase-4 (DPP-4) inhibitor that was approved in Japan in November 2012 for the treatment of patients with Type 2 diabetes mellitus (T2DM). Anagliptin (also known asSK-0403) is a treatment for diabetes based on inhibition of DPP-4, an enzyme that is responsible for degradation of glucagon-like peptide 1 (GLP-1), a 30-amino acid peptide that is secreted in response to food intake. GLP-1 stimulates insulin secretion and inhibits glucagon secretion, which leads to lower levels of plasma glucose. Following the introduction of the first DPP-4 inhibitor, sitagliptin, in 2006, several members of the gliptin class have been approved worldwide. Anagliptin was discovered from an effort to replace a metabolically labile isoindoline group from an earlier DPP-4 inhibitor series with a stable bioisostere. Anagliptin is a potent DPP-4 inhibitor, with an IC50=3.8 nM and >10,000-fold selectivity over inhibition of DPP-8 and DPP-9.
Originator
Sanwa Kagaku Kenkyusho (Japan)
Uses
Anagliptin is a dipeptidyl peptidase-4 (DPP-4) inhibitor that suppresses proliferation of vascular smooth muscles and monocyte inflammatory reaction. It also attenuates atherosclerosis in male apolipoprotein E-deficient mice.
Definition
ChEBI: Anagliptin is an amino acid amide.
brand name
Suiny
Clinical Use
Anagliptin, which is marketed as Beskoa or Suiny, is a dipeptidyl peptidase–IV (DPP-4) inhibitor which was approved in September 2012 and launched in November 2012 in Japan for the treatment of Type II diabetes. The drug was co-developed by three Japanese companies; Kowa, Sanwa Kagaku and JW pharmaceutical. Anagliptin, which is more selective against several recombinant human proteases by comparison to sitagliptin and vildagliptin, has more than 10,000-fold selectivity over the structurally homologous DPP-8 and DPP-9 enzymes.
Synthesis
The most likely process-scale synthesis has been published and is depicted in Scheme 3.24 Commercially available (S)-1-(2-chloroacetyl)-pyrrolidine-2-carbonitrile (12) was alkylated with t-butyl (2-amino-2-methyl-1-propyl)carbamate (13), giving rise to (S)-t-butyl (2-((2-(2-cyanopyrrolidin-1-yl)-2- oxoethyl)amino)-2-methylpropyl)carbamate (14). This Boc-protected system was subsequently treated with strong acid to give the ethylene diamine derivative 15 in 96% yield. Activation of 15 with CDI followed by coupling with commercially available 2-methylpyrazolo[1,5-a] pyrimidine-6-carboxylic acid (16) gave anagliptin (III) in 90% yield.
Anagliptin Preparation Products And Raw materials
Raw materials
Preparation Products
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View Lastest Price from Anagliptin manufacturers
- Product
- Anagliptin 739366-20-2
- Price
- US $5.00-0.10/KG
- Min. Order
- 1KG
- Purity
- 99%
- Supply Ability
- g-kg-tons, free sample is available
- Release date
- 2024-04-16
- Product
- Anagliptin 739366-20-2
- Price
- US $15.00-10.00/KG
- Min. Order
- 1KG
- Purity
- 99%+ HPLC
- Supply Ability
- Monthly supply of 1 ton
- Release date
- 2021-07-10
- Product
- Anagliptin 739366-20-2
- Price
- US $15.00-10.00/KG
- Min. Order
- 1KG
- Purity
- 99%+ HPLC
- Supply Ability
- Monthly supply of 1 ton
- Release date
- 2021-07-09