Title:
（５Ｓ，１０Ｓ）－１０－ベンジル－１６－メチル－１１，１４，１８－トリオキソ－１５，１７，１９－トリオキサ－２，７，８－トリチア－１２－アザヘンイコサン－５－アミニウム（Ｅ）－３－カルボキシアクリレート塩の調製のための工業的プロセス
Document Type and Number:
Japanese Patent JP6998864
Kind Code:
B2
Abstract:
The present invention relates to an industrial process for the preparation of (5S,10S)-10- benzyl-16-methyl-11,14,18-trioxo-15,17,19-trioxa-2,7,8-trithia-12-azahenicosan-5-aminium (E)-3-carboxyacrylate salt of following formula (I) : wherein X is fumarate. This process comprises the following successive key steps: a kinetic resolution, formation of disulfide compound, peptide coupling, and anion exchange reaction to obtain the desired product of formula (I).
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Inventors:
Polus Helve
Lefebvre Roi
Jao Shinjun
Ganberoni Luka
De Rosa Sabrina
Veraldi Rosario
Lefebvre Roi
Jao Shinjun
Ganberoni Luka
De Rosa Sabrina
Veraldi Rosario
Application Number:
JP2018519343A
Publication Date:
February 04, 2022
Filing Date:
October 14, 2016
Export Citation:
Assignee:
PHARMALEADS
International Classes:
C07C319/24; C07B57/00; C07C227/18; C07C229/08; C07C319/02; C07C319/28; C07C323/56; C07C327/32
Domestic Patent References:
| JP2009513600A | ||||
| JP2011522797A | ||||
| JP11228532A | ||||
| JP2005508308A |
Foreign References:
| US5552397 |
Other References:
BABAK KABOUDIN,RESOLUTION OF ENANTIOMERS OF NOVEL C2-SYMMETRIC AMINOBISPHOSPHINIC ACIDS VIA 以下備考,CHIRALITY,米国,2015年01月16日,VOL:27, NR:1,PAGE(S):71 - 74,http://dx.doi.org/10.1002/chir.22391,DIASTEREOMERIC SALT FORMATION WITH QUININE
CAMPBELL I G M,THE CHRYSANTHEMUMCARBOXYLIC ACIDS. IV. OPTICAL RESOLUTION OF THE CHRYSANTHEMIC ACIDS,JOURNAL OF THE SCIENCE OF FOOD AND AGRICULTURE,英国,WILEY & SONS,1952年04月,VOL:3,PAGE(S):189 - 192
Poras, Herve et al.,New Orally Active Dual Enkephalinase Inhibitors (DENKIs) for Central and Peripheral Pain Treatment,Journal of Medicinal Chemistry ,2014年,Vol.57(13),p.5748-5763
CAMPBELL I G M,THE CHRYSANTHEMUMCARBOXYLIC ACIDS. IV. OPTICAL RESOLUTION OF THE CHRYSANTHEMIC ACIDS,JOURNAL OF THE SCIENCE OF FOOD AND AGRICULTURE,英国,WILEY & SONS,1952年04月,VOL:3,PAGE(S):189 - 192
Poras, Herve et al.,New Orally Active Dual Enkephalinase Inhibitors (DENKIs) for Central and Peripheral Pain Treatment,Journal of Medicinal Chemistry ,2014年,Vol.57(13),p.5748-5763
Attorney, Agent or Firm:
Shimizu Hatsushi
Masao Haruna
Hirotaka Yamaguchi
Shun Jinbe
Ryuichi Inoue
Toshimitsu Sato
Koichi Niimi
Tomohiko Kobayashi
Hideki Kodera
Masato Ozeki
Kazuya Kawamoto
Masao Haruna
Hirotaka Yamaguchi
Shun Jinbe
Ryuichi Inoue
Toshimitsu Sato
Koichi Niimi
Tomohiko Kobayashi
Hideki Kodera
Masato Ozeki
Kazuya Kawamoto