Unii-950o97nupo Basic Product Information

Product Name	Unii-950o97nupo	CAS	377727-87-2
Synonyms	2-(2-Furanyl)-7-[2-[4-[4-(2-methoxyethoxy)phenyl]-1-piperazinyl]ethyl]-7H-pyrazolo[4,3-e][1,2,4]triazolo[1,5-c]pyrimidin-5-amine; Sch 420814	Molecular Formula	C25H29N9O3
EINECS Number		Molecular Structure
Appearance	Light Yellow Powder
Purity
Supply Ability

Unii-950o97nupo Quality documents

Unii-950o97nupo Appearance/Package/Shipping/Storage

package

storage condition

Store in cool & dry place,Keep away from strong light and heat

Unii-950o97nupo Application

Unii-950o97nupo literature

Fluorinated adenosine A_2A receptor antagonists inspired by preladenant as potential cancer immunotherapeutics

Yuan, Gengyang,Jankins, Tanner C.,Patrick, Christopher G.,Philbrook, Phaethon,Sears, Olivia,Hatfield, Stephen,Sitkovsky, Michail,Vasdev, Neil,Liang, Steven H.,Ondrechen, Mary Jo,Pollastri, Michael P.,Jones, Graham B.

, (2017)

Antagonism of the adenosine A_2A receptor on T cells blocks the hypoxia-adenosinergic pathway to promote tumor rejection. Using an in vivo immunoassay based on the Concanavalin A mouse model, a series of A_2A antagonists were studied and identified preladenant as a potent lead compound for development.Molecular modeling was employed to assist drug design and subsequent synthesis of analogs and those of tozadenant, including fluorinated polyethylene glycol PEGylated derivatives. The efficacy of the analogs was evaluated using two in vitro functional bioassays, and compound 29, a fluorinated triethylene glycol derivative of preladenant, was confirmed as a potential immunotherapeutic agent.

PROCESS AND INTERMEDIATES FOR THE PREPARATION OF PRELADENANT AND RELATED COMPOUNDS

-

, (2012/10/08)

The present invention describes processes for the synthesis of 2-(furan-2-yl)-7-[2-[4-[4-(2-methoxyethoxy)phenyl]piperazin-l-yl] ethyl]-7H-pyrazolo[ 4,3-e ][1,2,4]- triazolo[1,5c] pyrimidin-5-amine (Preladenant) represented by the structure of formula (1

Potent, selective, and orally active adenosine A_2A receptor antagonists: Arylpiperazine derivatives of pyrazolo[4,3-e]-1,2,4-triazolo[1,5-c]pyrimidines

Neustadt, Bernard R.,Hao, Jinsong,Lindo, Neil,Greenlee, William J.,Stamford, Andrew W.,Tulshian, Deen,Ongini, Ennio,Hunter, John,Monopoli, Angela,Bertorelli, Rosalia,Foster, Carolyn,Arik, Leyla,Lachowicz, Jean,Ng, Kwokei,Feng, Kung-I

, p. 1376 - 1380 (2008/02/05)

Antagonism of the adenosine A_2A receptor offers great promise in the treatment of Parkinson's disease. Employing the known pyrazolo[4,3-e]-1,2,4-triazolo[1,5-c]pyrimidine A_2A antagonist SCH 58261 as a starting point, we identified the potent and selective (vs. A1) antagonist 11 h, orally active in the rat haloperidol-induced catalepsy model. We further optimized this lead to the methoxyethoxyethyl ether 12a (SCH 420814), which shows broad selectivity, good pharmacokinetic properties, and excellent in vivo activity.

PROCESS FOR PREPARING SUBSTITUTED 5-AMINO-PYRAZOLO-[4,3-E]-1,2,4-TRIAZOLO[1,5-C]PYRIMIDINES

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Page/Page column 17, (2008/06/13)

A process for preparing substituted 5-amino-pyrazolo[4,3-e]-1,2,4-triazolo-[1,5-c]pyrimidine compounds having an aminoalkyl substituent at the 7-position is disclosed.

Unii-950o97nupo Upstream and downstream

377727-87-2 Upstream product

• 377729-82-3

  2-(5-amino-2-(furan-2-yl)-7H-pyrazole[4,3-e][1,2,4]triazole[1,5-c]pyrimidine-7-yl)ethyl 4-methylbenzenesulfonate 

• 515160-72-2

  1-(4-(2-methoxyethoxy)phenyl)piperazine 

• 3326-71-4

  2-furoic acid hydrazide 

• 39255-23-7

  1-Bromo-4-(2-Methoxyethoxy)-benzene 

• 5604-46-6

  2-amino-4,6-dichloropyrimidine-5-carboxaldehyde 

• 162401-16-3

  2-furan-2-yl-7H-pyrazolo[4,3-e]-1,2,4-triazolo[1,5-c]pyrimidin-5-yl amine 

• 377729-80-1

  furan-2-carboxylic acid N-(2-amino-6-chloro-5-formylpyrimidin-4-yl)-hydrazide 

• 377729-81-2

  furan-2-carboxylic acid N-(6-amino-1H-pyrazolo[3,4-d]pyrimidin-4-yl)-hydrazide 

377727-87-2 Downstream Products

• 377729-89-0

  C₁₆H₁₉N₉O 

• 1245905-29-6

  C₂₃H₂₇N₉O₃ 

• 1245905-32-1

  C₂₅H₂₉N₉O₅ 

• 1245905-31-0

  C₂₅H₂₉N₉O₅ 

• 1245905-33-2

  C₁₂H₁₂N₈O 

• 1245905-34-3

  C₂₅H₂₇N₉O₄ 

• 377727-88-3

  C₂₄H₂₅N₉O₃ 

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