111669-15-9

Upstream product

• 154117-92-7 2,4-dichloro-6-(pyrrolidin-1-yl)pyrimidine 
• 123-75-1 pyrrolidine 
• 3764-01-0 2,4,6-trichloropyrimidine 

Downstream Products

• 111641-17-9 2,4-bis(1-pyrrolidinyl)-6-(1-piperazinyl)-pyrimidine 
• 172035-68-6 U-101033 
• 262614-53-9 4-[4-(4-nitrophenyl)-1-piperazinyl]-2,6-di(1-pyrrolidinyl)pyrimidine 
• 157014-30-7 N-(4'-methoxyphenyl)-2,6-di-1-pyrrolidinyl-4-pyrimidinamine 
• 157012-37-8 6-phenyl-7-phenylmethyl-2,4-di-1-pyrrolidinyl-7H-pyrrolo[2,3-d]pyrimidine 
• 110101-66-1 16α-methyl-21-[4-[2,6-bis(1-pyrrolidinyl)-4-pyrimidinyl]-1-piperazinyl]-pregna-1,4,9(11)-triene-3,20-dione 
• 182146-03-8 7-methyl-6-(trifluoromethyl)-2,4-dipyrrolidinyl-7H-pyrrolo[2,3-d]pyrimidine 
• 157012-18-5 7-methyl-6-phenyl-2,4-di-1-pyrrolidinyl-7H-pyrrolo[2,3-d]pyrimidine 

Relevant academic research and scientific papers

Facile aromatic nucleophilic substitution (SNAr) reactions in ionic liquids: An electrophile-nucleophile dual activation by [Omim]Br for the reaction

A facile aromatic nucleophilic substitution (SNAr) reaction in recyclable [Omim]Br under relatively mild conditions has been described. An electrophile-nucleophile dual activation by [Omim]Br is also discovered based on control experiments, 1H NMR and IR spectroscopies. This chemistry provides an efficient and metal-free approach for the generation of Caryl-X (XS, N, O) bonds, many of which are significant synthetic intermediates or drugs, making this methodology attractive to both synthetic and medicinal chemistry.

TRIAMINOPYRIMIDINE DERIVATIVES AS INHIBITORS OF CDC25 PHOSPHATASE

The present invention relates to the novel triaminopyrimidine derivatives of formula (I) in which R1, R2, W, R3, R4, and R5 are variable groups. These products have a Cdc25-phosphatase-inhibiting activity. The invention also relates to a process for synth

TRIAMINOPYRIMIDINE CYCLOBUTENEDIONE DERIVATIVES USED AS PHOSPHATASE CDC25 INHIBITORS

The present invention relates to triaminopyrimidine derivatives of formula (I) where Y, R3, W, R4a, R5a, R4b, R5b, n and m are variable. These compounds have CDC25 phosphatase-inhibiting activity and can therefore be used as drugs in diseases in which CDC

Highly selective hydrolysis of chloropyrimidines to pyrimidones in 12 N hydrochloric acid

A chromatography-free process for synthesis of 6-piperazinyl-2,4-bis- pyrrolidinylpyrimidine in isomerically pure form is described. The key step is the purification of a crude 6-chloro-2,4-bis-pyrrolidinylpyrimidine/2-chloro-4, 6-bis-pyrrolidinylpyrimidine isomer mixture (generated by reaction of 2,4,6-trichloropyrimidine with pyrrolidine) by a highly selective acid-catalyzed hydrolysis of the 2-chloro isomer to the pyrimidone. The 2-chloro isomer hydrolyzes 350 times faster than the 6-chloro isomer in 6 N HCl and 1750 times faster in 12 N HCl. To put these rate ratios in perspective, the 2-chloro isomer reacts with amines and alkoxides only ～ 10-17 times faster than does the 6-chloro isomer. A mechanistic investigation using methodological tools developed by Bunnett established that the transition state for hydrolysis of the 6-chloro isomer involves two more molecules of water (each acting as a base) than does the transition state for hydrolysis of the 2-chloro isomer. As the concentration of HCl increases from 3 N to 6 N to 12 N, there are fewer unprotonated water molecules. Thus, the transition state that involves the greater number of unprotonated water molecules (6-chloro-2,4-bis- pyrrolidinylpyrimidine) is expected to be increasingly disfavored with increasing acid concentration, as is observed. The optimized process was run successfully on production scale.

Biologically active eburnamenine derivatives, pharmaceutical compositions containing them and process for preparing same

The invention relates to novel eburnamenine derivatives of formula (I): STR1 wherein R1 and R2 as well as R3 and R4, independently from each other, stand for hydrogen, C2-6 alkyl group, C2-6 alkenyl group; or a C3-10 alicyclic group involving 1 to 3 rings, and this latter group may be substituted by a C1-6 alkyl or C2-6 alkenyl group; or R1 and R2 and/or R3 and R4, together with the adjacent nitrogen atom and optionally with an additional oxygen or nitrogen atom, form a 4- to 6-membered, saturated or unsaturated cyclic group which may be substituted by a C1-6 alkyl or C2-6 alkenyl group; two of X, Y and Z are nitrogen whereas the third of them means a methine group; n is 1 or 2; W means oxygen or two hydrogen atoms; and the wavy line means α-/α-, α-/β- or β-/α- steric position, as well as their acid addition salts and solvates. The invention further relates to pharmaceutical compositions containing the above compounds as well as a process for preparing the compounds of formula (I). The compounds of formula (I) possess antioxidant effect and therefore, they are useful for inhibiting the peroxidation of lipids occurring in mammals (including human).

Amines useful in producing pharmaceutically active CNS compounds

Disclosed are Δ9(11) -steroids (VI) and amino substituted steroids (XI) which contain an amino group attached to the terminal carbon atom of the C17 -side chain, more particularly amino steroids (Ia and Ib), aromatic steroids (II), Δ16 -steroids (IIIa and IIIb), reduced A-ring steroids (IV), Δ17(20) -steroids (Va and Vb) and Δ9(11) -steroids (VI) which are useful as pharmaceutical agents for treating a number of conditions.

Pharmaceutically active amines

The aromatic amines (I), alkyl amines (II), bicyclic amines (III). STR1 cycloalkyl amines (IV), aromatic bicyclic amines (V), hydroquinone amines (VI), quinone amines (VII), amino-ethers (VIII) and bicyclic amino ethers (IX) are useful as pharmaceutical agents for treating a number of conditions including spinal trauma, mild and/or moderate to severe head injury, etc. Also disclosed is a method of treatment using the 3,4-dihydrobenzopyrans (XI).

Amino-9,10-secosteroids useful for treating head injury, spinal cord trauma or stroke

The amino-9,10-secosteroids STR1 of the present invention contain an amino group attached to the terminal carbon atom of the C17 -side chain and are useful as pharmaceutical agents for treating a number of conditions including spinal trauma, mild and/or moderate to severe head injury, etc.

Novel 21-Aminosteroids That Inhibit Iron-Dependent Lipid Peroxidation and Protect against Central Nervous System Trauma

A novel class of 21-aminosteroids has been developed.Compounds within this series are potent inhibitors of iron-dependent lipid peroxidation in rat brain homogenates with IC50's as low as 3 μM.Furthermore, selected members enhance early neurolo

C20 Through C26 amino steroids

Disclosed are Δ9 (11)-steroids (VI) and amino substituted steroids of formula (XI) which contain an amino group attached to the terminal carbon atom of the C17-side chain, more particularly amino steroids (Ia and Ib), aromatic steroids (II), Δ16 (11)-steroids (IIIa and IIIb), reduced A-ring steroids (IV), Δ17 (20)-steroids (Va and Vb) and Δ9 (11)-steroids (VI) which are useful as pharmaceutical agents for treating a number of conditions.