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US 6,605,744 B2Granted
Production of 2-amin-2-[2-(2-(40-C2-20-alkyl-phenyl)ethyl]propane-1,3-diols
AssigneesNovartis AG, Taito Co., Ltd., Mitsubishi Pharma Corporation
InventorsStephan Abel, Tetsuro Fujita, Ryoji Hirose, Guido Jordine, Tadashi Mishina
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Abstract
Disclosed is a process for the production of 2-amino-2-[2-(4-C2-20-alkyl-phenyl)ethyl]propane-1,3-diols.
Claims19
A process for preparing a 2-amino-2-[2-(4-C2-20alkylphenyl)ethyl]propane-1,3-diol, in free form or in salt form, which process comprises
- g) reducing a compound of formula (20)
- wherein R is C2-20alkyl, each of R1 and R2, independently, is C1-4alkyl and R3 is a protecting group,
- in the presence of (R4—CO)2O wherein R4 is C1-4alkyl, to obtain a compound of formula (21)
- wherein R, R3 and R4 are as defined above;
- and
- i) treating the resulting compound of formula (21) with a basic compound to obtain a compound of formula (22)
- wherein R is as defined above;
- and
- j) hydrogenating the resulting compound (22) and, where required, converting the resulting 2-amino-2-[2-(4-C2-20alkylphenyl)ethyl]propane-1,3-diol, into the desired salt form.
6 more elements
A process for the preparation of 2-amino-2-[2-(4-octylphenyl)-ethyl]propane-1,3-diol in free form or in salt form, comprising the step of reacting 2-(4-octylphenyl)ethyl bromide with diethyl acetamidomalonate.
Dependencies are inferred from the claim text.