87789-61-5

Usage

Uses

Used in Pharmaceutical Industry:
5-Benzyloxy-2-(1-piperazinyl)pyriMidine is used as a key intermediate in the synthesis of CNS agents for the treatment of various neurological and psychiatric disorders. Its unique structure allows for the development of compounds with specific binding affinities and selectivity for target receptors in the central nervous system, leading to potential therapeutic benefits.
As an intermediate in the preparation of CNS agents, 5-Benzyloxy-2-(1-piperazinyl)pyriMidine contributes to the advancement of pharmaceutical research and development. Its role in the synthesis of these agents is essential for creating effective treatments for a range of CNS-related conditions, ultimately improving the quality of life for patients suffering from these disorders.

InChI:InChI=1S/C15H18N4O/c1-2-4-13(5-3-1)12-20-14-10-17-15(18-11-14)19-8-6-16-7-9-19/h1-5,10-11,16H,6-9,12H2

Upstream product

• 110-85-0 piperazine 
• 138274-14-3 5-(benzyloxy)-2-chloropyrimidine 
• 99931-82-5 1-(5-bromopyrimidin-2-yl)piperazine 
• 100-51-6 benzyl alcohol 
• 100-39-0 benzyl bromide 

Downstream Products

• 1333320-39-0 N-{2-[4-(5-benzyloxy-pyrimidin-2-yl)-piperazin-1-yl]-2-oxo-ethyl}-2-fluoropyridine-4-carboxamide 
• 1333320-40-3 [⁽¹⁸⁾F]-N-{2-[4-(5-benzyloxy-pyrimidin-2-yl)-piperazin-1-yl]-2-oxo-ethyl}-2-fluoropyridine-4-carboxamide 
• 1333316-46-3 N-{2-[4-(5-benzyloxy-pyrimidin-2-yl)-piperazin-1-yl]-2-oxo-ethyl}-2-iodopyridine-4-carboxamide 
• 1333316-49-6 tert-butyl (2-{4-[5-(benzyloxy)pyrimidin-2-yl]piperazin-1-yl}-2-oxoethyl)carbamate 
• 106644-77-3 (1R*,2S*,3R*,4S*)-N-<4-<4-(5-Benzyloxy-2-pyrimidinyl)-1-piperazinyl>butyl>-2,3-bicyclo<2.2.1>heptanedicarboximide 

Relevant academic research and scientific papers

SPECT IMAGING AGENTS OF AMYLOID PLAQUES

The invention relates to novel iodine -radiolabeled compounds useful for diagnosing Alzheimer's desease, to respective novel precursors for the synthesis of such compounds, and to the process of manufacturing said imaging agent of the following Formula (I), wherein Q is a six membered aromatic ring, either carbocycle or heterocycle with one N- atom, wherein X1, X2, X3, X4 and X5 are independently selected from N or C, and wherein zero or one of X1 ( X2, X3, X4 or X5 is N and the remaining ones are C; A is either Sn(alkyl)3, I, l-123, l-124, l-125, l-131, Br; wherein alkyl comprises methyl, ethyl, propyl, butyl, pentyl and hexyl, Y is C or N; with the proviso that if X1 ( X2, X3, X4 or X5 has the meaning of N, substitution by A in that position is excluded; or a pharmaceutically acceptable salt thereof.

A NOVEL PET IMAGING AGENT OF AMYLOID PLAQUES AND ITS PRECURSOR

The invention relates to a [18F]-labeled PET tracer for imaging of Alzheimer's Disease, a suitable precursor for that PET tracer, and the process for preparing the respective [18F]-labeled PET tracer of the fol lowing Formula, wherein X is selected from the group consisting of: F, CI, Br, I, 18F, F, leaving groups, such as nitro and trimethyl ammonium, or a pharmaceutically acceptable salt thereof.

Synthesis and anxiolytic activity of N-substituted cyclic imides (1R*,2S*3R*,4S*)-N-[4-[4-(2-pyrimidinyl)-1-piperazinyl]butyl]-2,3-b icyclo[2.2.1]heptanedicarboxime (Tandospirone) and related compounds

A series of cyclic imides bearing a ω-(4-aryl and 4-heteroaryl-1-piperazinyl)alkyl moieties was synthesized and tested in vivo for anxiolytic activity. The in vitro binding affinities of these compounds were also examined for 5-HT(1A) receptor sites. Structure-activity relationships within these series are discussed. One of these compounds, (1R*,2S*,3R*,4S*)-N-[4-[4-(2-pyrimidinyl)-1-piperazinyl]butyl]-2,3- bicyclo[2.2.1]heptanedicarboximide (1: tandospirone), was found to be equipotent with buspirone in its anxiolytic activity and more anxio-selective than buspirone and diazepam. Tandospirone (1) is currently undergoing clinical evaluation as a selective anxiolytic agent.

Succinimide derivatives, and their production and use

A succinimide derivative of the formula: STR1 wherein R is a pyridyl or pyrimidinyl group substituted with at least one member selected from the group consisting of halogen, lower alkyl, lower alkoxy, cyano, benzyloxy, hydroxyl and amino, and n is an integer of 1 or 2, or a pharmaceutically acceptable acid addition salt thereof. The succinimide derivatives are useful as an anti-anxiety drugs.

2-[4-[(4,4-Dialkyl-2,6-piperidinedion-1-yl)butyl]-1-piperazinyl]pyrimidines

1-[4-(4,4-Dialkyl-2,6-piperidinedion-1-yl)butyl]piperazines with 2-pyrimidyl substituents in the 4- position have been synthesized and demonstrate useful anxiolytic properties. The compound 4,4-dimethyl-1-[4-[4-(2-pyrimidinyl)-1-piperazinyl]butyl]-2,6-piperidinedione, which has selective anxiolytic activity, constitutes the preferred embodiment of the invention.