Posatirelin

Base Information

Chemical Name:Posatirelin
CAS No.:78664-73-0
Molecular Formula:C₁₇H₂₈N₄O₄
Molecular Weight:352.434
Hs Code.:
UNII:78U6302ARL
DSSTox Substance ID:DTXSID301318172
Nikkaji Number:J153.926D
Wikidata:Q27266691
NCI Thesaurus Code:C74407
ChEMBL ID:CHEMBL2105243
Mol file:78664-73-0.mol

Synonyms:L-6-ketopiperidine-2-carbonyl-leucyl-proline amide;pAad-Leu-Pro-NH2;Piladox;posatirelin;posatireline;pyro-2-aminoadipoyl-leucyl-prolinamide;RGH 2202;RGH-2202

Suppliers and Price of Posatirelin

Supply Marketing:

Business phase:: The product has achieved commercial mass production^*data from LookChem market partment

Manufacturers and distributors:

Manufacture/Brand
Chemicals and raw materials
Packaging
price

Usbiological
Posatirelin
5mg
$ 305.00

TRC
Posatirelin
10mg
$ 770.00

American Custom Chemicals Corporation
N-[6-OXOPIPERIDIN-2(S)-YLCARBONYL]-L-LEUCYL-L-PROLINAMIDE 95.00%
5MG
$ 503.98

Total 5 raw suppliers

Chemical Property of Posatirelin

Chemical Property:

Vapor Pressure:9.66E-22mmHg at 25°C
Melting Point:214-216°
Boiling Point:739.6°C at 760 mmHg
Flash Point:401.1°C
PSA：129.57000
Density:1.214g/cm³
LogP:1.86610
XLogP3:-0.5
Hydrogen Bond Donor Count:3
Hydrogen Bond Acceptor Count:4
Rotatable Bond Count:6
Exact Mass:352.21105539
Heavy Atom Count:25
Complexity:549

Purity/Quality:

95% ^*data from raw suppliers

Posatirelin ^*data from reagent suppliers

Safty Information:

Pictogram(s):
Hazard Codes:

MSDS Files:: SDS file from LookChem

Useful:

Canonical SMILES:CC(C)CC(C(=O)N1CCCC1C(=O)N)NC(=O)C2CCCC(=O)N2
Isomeric SMILES:CC(C)C[C@@H](C(=O)N1CCC[C@H]1C(=O)N)NC(=O)[C@@H]2CCCC(=O)N2
Description Posatirelin is a TRH analogue. In a rat experimental model of brain cholinergic decit by lesion of the nucleus basalis magnocellularis (nbM), posatirelin treatment rescued cholinergic neurones of the nbM and their cholinergic projections to the cerebral cortex (Sabbatini et al., 1998). Posatirelin has been used in AD and VaD patients (Parnetti et al., 1995, 1996). VaD patients treated with posatirelin showed a signicant improvement in intellectual performance, orientation, motivation and memory as compared to controls. e drug was well tolerated.
Uses Posatirelin is a thyrotropin-releasing hormone analogue, used in the treatment of seizures and some neurodegenerative disease such as vascular dementia and Parkinson''s disease.

Technology Process of Posatirelin

There total 8 articles about Posatirelin which guide to synthetic route it. The literature collected by LookChem mainly comes from the sharing of users and the free literature resources found by Internet computing technology. We keep the original model of the professional version of literature to make it easier and faster for users to retrieve and use. At the same time, we analyze and calculate the most feasible synthesis route with the highest yield for your reference as below:

synthetic route:

Reference yield: 86.0%

: 78664-34-3
H-Leu-Pro-NH₂*HCl

: 78664-72-9
L-pyro-2-aminoadipic acid pentafluorophenyl ester

: 78664-73-0
L-pyro-2-aminoadipyl-L-leucyl-L-prolinamide

Guidance literature:: With triethylamine; In N,N-dimethyl-formamide; at 0 - 5 ℃; for 2h;
DOI:10.1021/jm00159a015

Reference yield:

: 6033-32-5
(S)-2-amino-6-hydroxyhexanoic acid

: 78664-73-0
L-pyro-2-aminoadipyl-L-leucyl-L-prolinamide

Guidance literature:: Multi-step reaction with 6 steps

1: 84 percent / aq. NaOH, aq. Na₂CO₃ / 3 h / 0 - 5 °C

2: 82 percent / aq. NaOH, KMnO₄ / 2 h / 5 - 10 °C

3: 83 percent / H₂, 60percent aq. AcOH / 10percent Pd/C / 2 h

4: 68 percent / 20percent aq. AcOH / 3 h / Heating

5: 92 percent / dicyclohexylcarbodiimide / ethyl acetate / 3 h / 0 - 5 °C

6: 86 percent / NEt₃ / dimethylformamide / 2 h / 0 - 5 °C

With sodium hydroxide; potassium permanganate; hydrogen; sodium carbonate; acetic acid; triethylamine; dicyclohexyl-carbodiimide; palladium on activated charcoal; In ethyl acetate; N,N-dimethyl-formamide;
DOI:10.1021/jm00159a015

Reference yield:

: 24325-14-2
(2S)-2-[(phenylmethoxy)carbonyl]aminoadipic acid

: 78664-73-0
L-pyro-2-aminoadipyl-L-leucyl-L-prolinamide

Guidance literature:: Multi-step reaction with 4 steps

1: 83 percent / H₂, 60percent aq. AcOH / 10percent Pd/C / 2 h

2: 68 percent / 20percent aq. AcOH / 3 h / Heating

3: 92 percent / dicyclohexylcarbodiimide / ethyl acetate / 3 h / 0 - 5 °C

4: 86 percent / NEt₃ / dimethylformamide / 2 h / 0 - 5 °C

With hydrogen; acetic acid; triethylamine; dicyclohexyl-carbodiimide; palladium on activated charcoal; In ethyl acetate; N,N-dimethyl-formamide;
DOI:10.1021/jm00159a015