221060-75-9

Upstream product

• 95-84-1 3-amino-4-hydroxytoluene 
• 221060-79-3 2-Bromo-5-methyl-3-thiophenecarbonyl chloride 
• 29421-92-9 4-bromo-2-methylthiophene 
• 19156-50-4 5-methyl-thiophene-3-carboxylic acid 
• 221061-14-9 2-bromo-5-methylthiophene-3-carboxylic acid 

Relevant academic research and scientific papers

Synthesis of thieno[2,3-b][1,5]benzoxazepine derivatives

A new series of 4-(4-methylpiperazin-1-yl)thieno[2,3-b][1,5]benzoxazepines 1a-k has been synthesized from 4-bromo-2-methylthiophene 6 or ethyl 2-amino-4,5-dimethyl-3-thiophencarboxylate 10. Preparation of the key intermediate thieno[2,3-b][1,5]benzoxazepine-4(5H)-ones 4a-i, 4k were carried out by treatment of 2-bromo-N-(2-hydroxyphenyl)-3-thiophencarboxamides 5a-i, 5k with potassium carbonate in DMSO. Compounds 1 are thienoanalogues of loxapine, a potent antipsychotic drug. Of these compounds, the neuroleptic activity of 2-methyl-4-(4-methylpiperazin-1-yl)thieno[2,3-b][1,5]benzoxazepine 1a (R1, R3=H, R2=CH3) demonstrated potent antipsychotic activity.

Fused thiophene compounds and medicinal use thereof

A condensed thiophene compound of the formula (I) wherein each symbol is as defined in the specification, a pharmaceutically acceptable salt thereof and hydrates thereof. The compound of the formula (I) of the present invention is useful as a novel antipsychotic agent which is effective for both positive symptoms and negative symptoms of schizophrenia, which is associated with less side effects such as extrapyramidal motor disorder and the like and which is less associated with serious side effects such as agranulocytosis and the like. In addition, this compound is also useful as a therapeutic agent of Alzheimer's disease and manic-depressive illness.