Some content of this application is unavailable at the moment.
If this situation persist, please contact us atFeedback&Contact
1. (WO2018059279) METHOD FOR SYNTHESIZING NOVEL CHIRAL LIGAND, METAL CHELATE, A VARIETY OF NON-NATURAL AMINO ACIDS, MARAVIROC AND KEY INTERMEDIATE THEREOF
Latest bibliographic data on file with the International Bureau    Submit observation

Pub. No.: WO/2018/059279 International Application No.: PCT/CN2017/102327
Publication Date: 05.04.2018 International Filing Date: 19.09.2017
IPC:
C07D 207/16 (2006.01) ,C07D 409/12 (2006.01) ,C07F 15/04 (2006.01) ,C07C 227/34 (2006.01) ,C07C 229/34 (2006.01) ,C07D 401/04 (2006.01)
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
207
Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
02
with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
04
having no double bonds between ring members or between ring members and non-ring members
10
with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
16
Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
409
Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
02
containing two hetero rings
12
linked by a chain containing hetero atoms as chain links
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
F
ACYCLIC, CARBOCYCLIC, OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
15
Compounds containing elements of the 8th Group of the Periodic System
04
Nickel compounds
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
C
ACYCLIC OR CARBOCYCLIC COMPOUNDS
227
Preparation of compounds containing amino and carboxyl groups bound to the same carbon skeleton
30
Preparation of optical isomers
34
by separation of optical isomers
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
C
ACYCLIC OR CARBOCYCLIC COMPOUNDS
229
Compounds containing amino and carboxyl groups bound to the same carbon skeleton
02
having amino and carboxyl groups bound to acyclic carbon atoms of the same carbon skeleton
34
the carbon skeleton containing six-membered aromatic rings
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
401
Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
02
containing two hetero rings
04
directly linked by a ring-member-to-ring- member bond
Applicants:
中国科学院上海药物研究所 SHANGHAI INSTITUTE OF MATERIA MEDICA, CHINESE ACADEMY OF SCIENCES [CN/CN]; 中国上海市 浦东张江祖冲之路555号 555 Zu Chong Zhi Road, Zhang Jiang, Pudong Shanghai 201203, CN
Inventors:
柳红 LIU, Hong; CN
王江 WANG, Jiang; CN
周圣斌 ZHOU, Shengbin; CN
彭攀峰 PENG, Panfeng; CN
年永 NIAN, Yong; CN
王姝妮 WANG, Shuni; CN
舒双杰 SHU, Shuangjie; CN
沈昊 SHEN, Hao; CN
蒋华良 JIANG, Hualiang; CN
陈凯先 CHEN, Kaixian; CN
Agent:
上海一平知识产权代理有限公司 XU & PARTNERS,LLC.; 中国上海市 普陀区真北路958号天地科技广场1号楼106室 Room No.106, Building No.1, Universal High-Tech Plaza, 958 Zhen Bei Road, Putuo District Shanghai 200333, CN
Priority Data:
201610871043.629.09.2016CN
Title (EN) METHOD FOR SYNTHESIZING NOVEL CHIRAL LIGAND, METAL CHELATE, A VARIETY OF NON-NATURAL AMINO ACIDS, MARAVIROC AND KEY INTERMEDIATE THEREOF
(FR) PROCÉDÉ DE SYNTHÈSE D'UN NOUVEAU LIGAND CHIRAL, CHÉLATE MÉTALLIQUE, VARIÉTÉ D'ACIDES AMINÉS NON NATURELS, MARAVIROC ET INTERMÉDIAIRE CLÉ DE CELUI-CI
(ZH) 新型手性配体、金属螯合物、多种非天然氨基酸、马拉维诺及其关键中间体的合成方法
Abstract:
(EN) Disclosed is a method for synthesizing a novel chiral ligand, a metal chelate, a variety of non-natural amino acids, Maraviroc and a key intermediate thereof. In the invention, (R)-2-methyl proline is selected and used as a starting raw material, (S)-β3-amino acid is obtained by asymmetric resolution induced by using a nickel chelate, and Maraviroc is synthesized by using (S)-3-amino-3-phenylpropionic acid as a key intermediate with a high yield and the ee value reaching 98.2% or more. The method of the present invention has widely available materials, mild synthetic process conditions, is easy to control, and produces a product of a high optical purity.
(FR) L'invention concerne un procédé de synthèse d'un nouveau ligand chiral, d'un chélate métallique, d'une variété d'acides aminés non naturels, de Maraviroc et d'un intermédiaire clé de celui-ci. Selon l'invention, la (R)-2-méthyl-proline est sélectionnée et utilisée en tant que matière première de départ, l'acide aminé (S)-bêta 3 - est obtenu par une résolution asymétrique induite par l'utilisation d'un chélate de nickel, et le Maraviroc est synthétisé en utilisant (S)-3-amino-3-phénylpropionique en tant qu'intermédiaire clé avec un rendement élevé et la valeur ee atteignant 98,2 % ou plus. Le procédé de la présente invention présente des matériaux largement disponibles, des conditions de traitement de synthèse modérées, est facile à commander, et fourni un produit d'une pureté optique élevée.
(ZH) 本发明公开了一种新型手性配体、金属螯合物、多种非天然氨基酸、马拉维诺及其关键中间体的合成方法,本发明选用(R)-2-甲基脯氨酸为起始原料,利用镍螯合物诱导不对称拆分获得(S)-β3-氨基酸,并以(S)-3-氨基-3-苯基丙酸作为关键中间体,合成马拉维诺,收率高,且ee值达到98.2%以上。本发明的方法,原料来源广泛,合成工艺条件温和,易于控制,产品光学纯度高。
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: Chinese (ZH)
Filing Language: Chinese (ZH)