Some content of this application is unavailable at the moment.
If this situation persist, please contact us atFeedback&Contact
1. (WO2019049918) INDUSTRIAL PROCESS OF MONO-ALKYLATING A PIPERIDINE NITROGEN IN PIPERIDINE DERIVATIVES WITH DEUTERATED-ALKYL
Latest bibliographic data on file with the International Bureau    Submit observation

Pub. No.: WO/2019/049918 International Application No.: PCT/JP2018/032983
Publication Date: 14.03.2019 International Filing Date: 06.09.2018
IPC:
C07D 221/28 (2006.01) ,C07B 59/00 (2006.01)
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
221
Heterocyclic compounds containing six-membered rings having one nitrogen atom as the only ring hetero atom, not provided for by groups C07D211/-C07D219/187
02
condensed with carbocyclic rings or ring systems
22
Bridged ring systems
28
Morphinans
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
B
GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
59
Introduction of isotopes of elements into organic compounds
Applicants:
OTSUKA PHARMACEUTICAL CO., LTD. [JP/JP]; 2-9, Kanda Tsukasa-machi, Chiyoda-ku, Tokyo 1018535, JP
Inventors:
NAKAI, Yuya; JP
HAYASHI, Masashi; JP
MITSUHASHI, Wataru; JP
Agent:
YAMAO, Norihito; JP
SHINAGAWA, Hisatoshi; JP
Priority Data:
2017-17235107.09.2017JP
Title (EN) INDUSTRIAL PROCESS OF MONO-ALKYLATING A PIPERIDINE NITROGEN IN PIPERIDINE DERIVATIVES WITH DEUTERATED-ALKYL
(FR) PROCÉDÉ INDUSTRIEL DE MONOALKYLATION D'UN AZOTE DE PIPÉRIDINE DANS DES DÉRIVÉS DE LA PIPÉRIDINE AVEC UN ALKYLE DEUTÉRÉ
Abstract:
(EN) The present invention relates to a method of mono-alkylating a piperidine nitrogen in a piperidine derivative with a deuterated lower-alkyl, which comprises protecting the piperidine nitrogen with an aralkyl protective group, lower-alkylating the piperidine nitrogen with a deuterated-lower-alkylating agent under neutral or basic condition, and then deprotecting the aralkyl protective group.
(FR) La présente invention concerne un procédé de monoalkylation d'un azote de pipéridine dans un dérivé de la pipéridine avec un alkyle inférieur deutéré, qui consiste à protéger l'azote de la pipéridine avec un groupe protecteur aralkyle, à alkyler à l'aide d'un alkyle inférieur l'azote de la pipéridine avec un agent alkylant à alkyle inférieur deutéré dans des conditions neutres ou basiques, puis à déprotéger le groupe protecteur aralkyle.
front page image
Designated States: AE, AG, AL, AM, AO, AT, AU, AZ, BA, BB, BG, BH, BN, BR, BW, BY, BZ, CA, CH, CL, CN, CO, CR, CU, CZ, DE, DJ, DK, DM, DO, DZ, EC, EE, EG, ES, FI, GB, GD, GE, GH, GM, GT, HN, HR, HU, ID, IL, IN, IR, IS, JO, JP, KE, KG, KH, KN, KP, KR, KW, KZ, LA, LC, LK, LR, LS, LU, LY, MA, MD, ME, MG, MK, MN, MW, MX, MY, MZ, NA, NG, NI, NO, NZ, OM, PA, PE, PG, PH, PL, PT, QA, RO, RS, RU, RW, SA, SC, SD, SE, SG, SK, SL, SM, ST, SV, SY, TH, TJ, TM, TN, TR, TT, TZ, UA, UG, US, UZ, VC, VN, ZA, ZM, ZW
African Regional Intellectual Property Organization (ARIPO) (BW, GH, GM, KE, LR, LS, MW, MZ, NA, RW, SD, SL, ST, SZ, TZ, UG, ZM, ZW)
Eurasian Patent Office (AM, AZ, BY, KG, KZ, RU, TJ, TM)
European Patent Office (EPO) (AL, AT, BE, BG, CH, CY, CZ, DE, DK, EE, ES, FI, FR, GB, GR, HR, HU, IE, IS, IT, LT, LU, LV, MC, MK, MT, NL, NO, PL, PT, RO, RS, SE, SI, SK, SM, TR)
African Intellectual Property Organization (BF, BJ, CF, CG, CI, CM, GA, GN, GQ, GW, KM, ML, MR, NE, SN, TD, TG)
Publication Language: English (EN)
Filing Language: English (EN)