Dauzonne et al. (1995) had reported the synthesis and some CNS activities of new benzofuranyl acryloylpiperazine. This literature describes our attempts to explore the pharmacological properties related to chemical modifications carried on a new series of (E)-4-[3-(2-benzofuranyl) acryloyl] piperazine (fig.24), obtained as their hydrochloride, substituted at N-1 and benzofuran ring in various ways.
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INTRODUCTION: One of the main objectives of organic and medicinal chemistry is the design, synthesis and production of molecules having value as human therapeutic agents. During the past decade, Combinatorial chemistry has provided access to chemical libraries based on privileged structures 1, with heterocyclic structures receiving special attention as they belong to a class of compounds with proven utility in medicinal chemistry 2. Piperazine which arrived in the 1950 was the first modification with broad spectrum activity. Useful in the ascarides, small strongyles and pinworms. It still wasn’t effective against the large strongyles. 3
Paraben（Methyl, Ethyl, Propyl, Butyl）
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CONCLUSION: The article has outlined the chemistry and biological activities of the piperazine scaffold. The synthetic methodologies indicate the simplicity, maneuverability and versatility, which offer the medicinal chemist a complete range of novel derivatives. The stereochemical orientation provides a further variety of products. The high degree of protection against seizures can be positive signs for further investigation of piperazine derivatives as anticonvulsants. The activity of piperazine as antihistaminic and their potent anthelmintic activity are promising. The broad spectrum antibacterial and antifungal activity of these compounds could lead to a new series of antimicrobials. The piperazine derivatives have demonstrated significant antidiabetic and antiproliferative activities. Thus piperazine scaffold is not only synthetically important but also possesses a wide range of promising biological activities.
Find methyl butyl ether at GFS Chemicals: ..
Kossakowski et al. (2006) described the preparation of a no. of cyclic imide 5-HT1A receptor ligand derivatives. Their structures were conformationally constrained by introducing rigid linkers containing unsaturated bonds or aromatic benzene ring. These compounds are expected to possess anxiolytic and antidepressant activity. Linkers are cis- and trans-1,4-dichloro-2-butene, 1,2 – bis (chloromethyl)benzene, 1 - (2-methoxy phenyl) piperazine.
chlorohydrin UN 2612 3 Methyl propyl ether UN ..
2.4.3 Alkylation of Piperazine: 15 Piperazine is generally alkylated to yield the N, N’-disubstituted compounds. It is possible to prepare monoalkylated piperazine by first blocking one nitrogen with ethyl chloroformate, reaction of the other nitrogen with an alkyl halide, and hydrolyzing to liberate the monoalkylated compound.
Parabens (Methyl-, Ethyl-, Propyl-, ..
Method: The chiral bislactim ether is converted into the anion (under kinetic control) by rc-butyllithium. Alkylation proceeds with high stereoselectivity (greater than 95%). Acid hydrolysis of the alkylation leads to (unnatural) (R)-amino acids and recovery of the chiral auxiliary valine, from which the start dioxopiperazine was derived.
beta-dimethylaminoethyl benzhydryl ether
2.4.2 O-Alkylation 14 O-Alkylation of dioxopiperazines with oxonium salts yields bislactim ethers which are used as reagents for the asymmetric synthesis of amino acids (Fig. 9).