Mitsubishi Chemical Industries Limited

Mitsubishi Petrochemical Company Limited

Kabushiki Kaisha Cosmos Enterprise

Sanyo Fine Co., Ltd.

Yoshitaka Sako

Bompei Yasui

Takashi Kurihara

Tomohisa Miyamoto

Sachio Hirose

Hidenari Adachi

Tammotsu Homma

Katsuyuki Hiraoka

Makiko Shibata

There are disclosed a novel polypeptide represented by the formula shown below or its acid addition salt or complex: ##STR1## wherein Ala represents alanine, Ser serine, Leu leucine, Thr threonine, Val valine, Gly glycine, Lys lysine, Gln glutamine, Glu glutamic acid, His histidine, Tyr tyrosine, Pro proline, Arg arginine, Asp aspartic acid, and n represents an integer of 3 to 7, and a process for producing the same comprising forming a peptide or polypeptide represented by the above formula and subjecting the structural units containing a peptide residue represented by the formula: ##STR2## wherein R represents an active ester residue, Ala, Ser, Leu, Thr and n have the same meanings as defined above, formed in any step of the reaction to cyclization reaction.

Novel polypeptide and process for producing the same

A process for the preparation of 1-(4-hydroxyphenyl)-2-(4-benzylpiperidino)-1-propanol (i.e. ifenprodil) and acid-addition salts thereof, characterized by brominating 4'-hydroxypropiophenone in a single or mixed solvent selected from the group consisting of methanol, ethanol and a saturated aliphatic ether, removing hydrogen bromide formed in the course of the bromination, adding 4-benzylpyridine to the reaction mixture, heating the reaction mixture under reflux in a single or mixed solvent selected from the group consisting of methanol and ethanol, and then subjecting the resultant reaction mixture to catalytic reduction to form 1-(4-hydroxyphenyl)-2-(4-benzylpiperidino)-1-propanol hydrobromide in the reaction mixture. The end product (i.e. ifenprodil) can be obtained according to this process in a high yield of about 80% within 14 hours from the starting material in a single reaction container throughout the process, without introducing a protective benzyl group into the starting material prior to the bromination.

Process for the preparation of

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Osaka, Japan

Yoshitaka Sako