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Pub. No.:    WO/2013/058241    International Application No.:    PCT/JP2012/076710
Publication Date: 25.04.2013 International Filing Date: 16.10.2012
C07C 213/10 (2006.01), C07B 53/00 (2006.01), C07B 57/00 (2006.01), C07C 59/50 (2006.01), C07C 213/00 (2006.01), C07C 215/08 (2006.01), C07B 61/00 (2006.01)
Applicants: KANEKA CORPORATION [JP/JP]; 3-18, Nakanoshima 2-chome, Kita-ku, Osaka-shi, Osaka 5308288 (JP)
Inventors: YOSHIDA, Fumi; (JP).
HIRAI, Yoshinori; (JP).
Agent: UEKI, Kyuichi; Fujita-Toyobo Building 9th floor, 1-16, Dojima 2-chome, Kita-ku, Osaka-shi, Osaka 5300003 (JP)
Priority Data:
2011-229047 18.10.2011 JP
(JA) (R)-2-アミノ-2-エチルヘキサノールの製造法
Abstract: front page image
(EN)The present invention makes it possible to produce (R)-2-amino-2-ethylhexanol, which is useful as a pharmaceutical intermediate, easily and efficiently without complicated procedures. (R)-2-amino-2-ethylhexanol is produced by asymmetrical alkylation of an N-benzylidene-2-aminoester derivative using an optically active phase-transfer catalyst, followed by debenzylidenation, reduction, and the like. Additionally, a solid (R)-2-amino-2-ethylhexanol salt is obtained and the optical purity is improved by forming a salt with an optically active acid and precipitating a solid.
(FR)Cette invention permet d'obtenir un (R)-2-amino-2-éthylhexanol de manière facile et efficace, sans procédures compliquées, qui est utile en tant qu'intermédiaire pharmaceutique. Le (R)-2-amino-2-éthylhexanol selon l'invention est obtenu par alkylation asymétrique d'un dérivé de N-benzylidène-2-aminoester à l'aide d'un catalyseur de transfert de phase optiquement actif, puis débenzilidénation, réduction et autre. De plus, un sel de (R)-2-amino-2-éthylhexanol solide est obtenu et sa pureté optique est améliorée par formation d'un sel avec un acide optiquement actif et précipitation d'un solide.
(JA) 煩雑な操作を行うことなく、簡便且つ効率的に医薬品中間体として有用な(R)-2-アミノ-2-エチルヘキサノールを製造する。N-ベンジリデン-2-アミノエステル誘導体に、光学活性な相間移動触媒を用いて不斉アルキル化を行い、続いて脱ベンジリデン化、還元などを行うことにより(R)-2-アミノ-2-エチルヘキサノールを製造する。更に、光学活性な酸と塩を形成させて固体を析出させることにより、(R)-2-アミノ-2-エチルヘキサノール塩の固体を取得して光学純度を向上させる。
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, DK, DM, DO, DZ, EC, EE, EG, ES, FI, GB, GD, GE, GH, GM, GT, HN, HR, HU, ID, IL, IN, IS, JP, KE, KG, KM, KN, KP, KR, KZ, LA, LC, LK, LR, LS, LT, 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, 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 (BW, GH, GM, KE, LR, LS, MW, MZ, NA, RW, SD, SL, SZ, TZ, UG, ZM, ZW)
Eurasian Patent Organization (AM, AZ, BY, KG, KZ, RU, TJ, TM)
European Patent Office (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, ML, MR, NE, SN, TD, TG).
Publication Language: Japanese (JA)
Filing Language: Japanese (JA)