Perazine

Pentazocine j, 297 2 325 Pentobarbital 1, 268 Pentomone 3, 2T8 PentoxphylTine 466 Pentyl enetetrazole 281 Perazine 1, 381 Pergolide 249 Perlapine 425 Perphenazine 1, 383 Pethidine 1, 300 Phenacaine 19 Phenacemide 1, 95 Phenacetemide Phenacetin 111... 

C (H 7C1N2 104-16-5) see Butaperazine Perazine Prochlorperazine Thiethylperazine Thioproperazine Trifluoperazine... 

C,2Hi,NS 92-84-2) see Alimemazine Aminopromazine Dimethoxanate Dixyrazine Fenoverine Mequitazine Methdilazine Oxomemazine Pecazine Perazine Profenamine Promazine Promethazine Propyramazine... 

Silylation of amino acids such as r-leucine 180 with TCS 14 gives rise to the O-silylated ammonium salt 181, which reacts selectively with triphosgene and triethylamine to afford the isocyanate 182. Subsequent reaction of 182 with primary amines such as free r-leucine 180 or secondary amines such as N-BOC-pi-perazine 184 affords the ureas 183 and 185 in 49% or 77% overall yield, respectively [10] (Scheme 4.7). 

The final method for constructing epidithiodiketopiperazine motifs relied on the nucleophilic thiolation of /V-acyliminium ions. Access to alpha-oxidized diketopi-perazine structures was central to this approach, and key developments were made in this regard. Schmidt first demonstrated the feasibility of this ionization approach in 1973 by conversion of proline anhydride to its diacetate using Pb(OAc)4 [42], Hydrolysis of the acetates, ionization of the hemiaminals with zinc chloride in the presence of hydrogen sulfide, and oxidation with iodine provided the epidisulfide of interest. In 1975, Matsunari reported access to alpha-methoxy diketopiperazines,... 

Odontiadis J, Franklin M. 1996. Simultaneous quantitation of buspirone and its major metabolite l-(2-pyrimidinyl)pi-perazine in human plasma by high-performance liquid chromatography with coulometric detection. J Pharm Biomed Anal 14(3) 347-351. 

The scope and limitations of the solid-supported symthesis of bicyclic diketopi-perazines 165 as peptide p-tum mimetic were further investigated by Golebiowski et al. [52]. The four-component Ugi reaction of a-iV-Boc-diaminopropionic acid resin ester 160 (an amine input) and optically active a-bromoacid 163 with various isocyanides 166 and aldehydes 167 yields a series of bicyclic diketopiperazines 165 (Scheme 28). 

The piperazines include fluphenazine, trifluoperazine, prochlorperazine, perazine and perphenazine. They are agents with a high antipsychotic potency with less pronounced anticholinergic effects. However their potential to produce extrapyramidal effects is more pronounced. 

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