Haloperidol is one of the most actively used modern neuroleptics. Its high antipsychotic activity is combined with a moderate sedative effect. It effectively stops various types of psychomotor excitement. It is used for schizophrenic psychoses, manic, paranoid, and delirious conditions, depression, psychomotor excitement of various origins, and for delirium and hallucinations of different origin. The most common synonyms are haldol, vezadol, linton, and others.

Droperidol: Droperidol, 1-[1-[3-(p-fluorobenzoyl)propyl]-1,2,3,6,4-piridyl]-2-benzymi-dazolinone (6.3.11), is synthesized from 1-benzyl-3-carbethoxypiperidin-4-one (3.1.47), which is reacted with o-phenylendiamine. Evidently, the first derivative that is formed under the reaction conditions, 1,5-benzdiazepine, rearranges into 1-(1-benzyl-1,2,3,6-tetrahydro-4-piridyl)-2-benzymidazolone (6.3.9). Debenzylation of the resulting product with hydrogen over a palladium catalyst into 1-(1,2,3,6-tetrahydro-4-piridyl)-2-benzimi-dazolon (6.3.10) and subsequent alkylation of this using 4'-chloro-4-fluorobutyrophenone (6.3.4) yields droperidol (6.3.11) [47-49].

cooc2h5 o

/—{ JJ^ h2/ Pd—C CH2—+ ^^^ -*" ^ ß— CH2—N y-N N-H ->

The neuroleptic droperidol possesses antipsychotic, sedative, and antishock action. It potentiates the action of drugs for narcosis. In psychiatric practice, droperidol is used for psychomotor excitement and hallucinations. The principal use of this drug lies in anesthesiology for neuroleptanalgesia in combination with fentanyl. It is used in premedication as well as in surgical operations and post-operational circumstances. Synonyms of this drug are talam-onal, droleptan, leptofen, innovar, and others.

Fluanisone: Fluanisone, 4'-fluoro-4-[4-(o-methoxyphenyl)-1-piperazinyl]-butyrophe-none (6.3.12), is synthesized by reacting 1-(2'-methoxyphenyl)-piperazine with 4'-chloro-4'-fluorobutyrophenone (6.3.4) [50].



Fluanisone is a neuroleptic with sedative properties and relatively poorly expressed antipsychotic action. It is used as an independent or adjuvant drug for psychomotor excitement in severe and chronic schizophrenia and for manic-depressive disorder. Synonyms of this drug are sedalande, methorin, and others.

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