- Preparation method of L-phenylephrine hydrochloride
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The invention relates to a preparation method of L-phenylephrine hydrochloride, and specifically discloses a preparation method of L-phenylephrine hydrochloride, which comprises the steps of chlorination reaction, chiral reduction reaction, amination salifying and recrystallization. The preparation method has the advantages of cheap and easily available raw materials, simple operation process, loweconomic cost, high product yield and the like, and the product quality meets the standard requirements of Chinese Pharmacopoeia and European Pharmacopoeia.
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Paragraph 0078-0086
(2020/10/04)
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- Efficient synthesis of (R)-phenylephrine using a polymer-supported Corey-Bakshi-Shibata catalyst
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An efficient and mild synthetic route to (R)-phenylephrine hydrochloride using Corey-Bakshi-Shibata (CBS) catalyst was reported. In order to avoid a lengthy recovery process of the catalyst from homogeneous reaction, a polymer-supported CBS catalyst was prepared, and a preliminary attempt was made to achieve a continuous reduction on a laboratory scale, which contributes to synthesis of (R)-phenylephrine in a cost-effective way.
- Dai, Shuangxiong,Li, Guohua,Zhang, Wenbo,Zhang, Cuiyan,Song, Xiaoling,Huang, Di
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p. 740 - 743
(2017/05/16)
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- PROCESS FOR RESOLUTION OF 1-(3-HYDROXYPHENYL)-2-METHYLAMINO ETHANOL
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Resolution of the title compound to its active isomer (R)-1-(3-hydroxyphenyl)-2-methylamino ethanol with (R)-naproxen as a resolving agent.
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- A feasibility study on the synthesis of phenylephrine via ruthenium-catalyzed homogeneous asymmetric hydrogenation
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We report a feasibility study on a new route to (R)-phenylephrine, based on the ruthenium-catalyzed asymmetric hydrogenation of an aminoketone precursor. The direct and fast asymmetric reduction of aminoketones or their hydrochloride salts is achievable at low catalyst loadings (molar substrate to catalyst ratio, S/C, >25,000/1, TOF up to 25,000 h-1) with high enantioselectivity (>95% ee), without the need for N-protection nor isolation of the free base prior to reaction.
- McGarrity, John F.,Zanotti-Gerosa, Antonio
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experimental part
p. 2479 - 2486
(2011/02/22)
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- PROCESS FOR THE PREPARATION OF OPTICALLY ACTIVE 2-AMINO-1-PHENYLETHANOLS
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Optically active 2-amino-l-phenylethanols of formula (I) or its mirror image, wherein R1 is C1-6 alkyl or aryl-substituted C1-6 alkyl and R2 through R6 are independently hydrogen, hydroxy or C1-6 alkoxy, or salts thereof are prepared by asymmetric hydrogenation of the corresponding 2-aminoaceto-phenones in the presence of a rhodium complex catalyst comprising a chiral diphosphine ligand, wherein each phosphorus atom is part of a heterocyclic ring system which contains at least one chiral carbon atom directly bound to the phosphorus atom.
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Page/Page column 14
(2008/12/08)
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- PROCESS FOR THE PREPARATION OF OPTICALLY ACTIVE 2-AMINO-1-PHENYLETHANOLS
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Optically active 2-amino-l-phenylethanols of formula (I) or its mirror image, wherein R1 is hydrogen, C1-6alkyl or aryl-substituted C1-6alkyl and R2 through R6 are independently hydrogen, hydroxy or C1-6alkoxy, or salts thereof are prepared by asymmetric hydrogenation of the corresponding 2-aminoacetophenones in the presence of a ruthenium complex catalyst comprising a chiral phosphine ligand.
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Page/Page column 12
(2008/12/06)
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- Oral pharmaceutical compositions containing cyclodextrins as taste masking agent
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The application discloses oral pharmaceutical compositions which are tasted in the mouth during administration. Fast-dissolving tablets, chewable tablets and effervescent dispersions are exemplified. To mask the taste of unpleasant-tasting active ingredients, it has been found that blending with cyclodextrin without the conventional complex formation is effective. Consequently more economical modes of manufacture such as simple granulation and dry blending can be used.
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- Enantioselective synthesis of (R)-phenylephrine hydrochloride
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An efficient method for the synthesis of enantiomerically pure (R)-phenylephrine hydrochloride 1 is described using a Sharpless asymmetric dihydroxylation as the key step.
- Pandey, Rajesh Kumar,Upadhyay, Puspesh Kumar,Kumar, Pradeep
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p. 6245 - 6246
(2007/10/03)
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- Method for preparing of L-phenylephrine hydrochloride
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The present invention relates to an improved process for preparing L-phenylephrine hydrochloride 3 on an industrial scale by asymmetric hydrogenation as the key step and a special sequence of subsequent steps, using [Rh(COD)Cl]2 as catalyst and a chiral, two-pronged phosphine ligand such as (2R,4R)-4-(dicyclohexylphosphino)-2-(diphenylphosphino-methyl)-N-methyl-aminocarbonyl-pyrrolidine as the catalyst system.
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- A practical synthesis of (R)-(-)-phenylephrine hydrochloride
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(R)-(-)-Phenylephrine hydrochloride is a clinically potent adrenergic agent and β-receptor sympathomimetic drug, exclusively marketed in the optically active form. An asymmetric synthesis has been developed with high enantiomeric excess based on hydrolytic kinetic resolution of a styrene oxide derivative using (R,R)-SalenCoIIIOAc complex.
- Gurjar, Mukund K.,Krishna, L. Murali,Sarma, Bugga V.N.,Chorghade, Mukund S.
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p. 422 - 424
(2013/09/08)
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- Efficient asymmetric hydrogenation of α-amino ketone derivatives. A highly enantioselective synthesis of phenylephrine, levamisole, carnitine and propranolol
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The complexes of pyrrolidine bisphosphine ligands (CPMs) with rhodium (I) were found to be efficient catalysts for asymmetric hydrogenation of α-amino ketone hydrochloride derivatives. Utilizing this methodology, we have developed efficient asymmetric syntheses of the optically active β-amino alcohols, phenylephrine, levamisole, carnitine and propranolol.
- Sukuraba,Takahashi,Takeda,Achiwa
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p. 738 - 747
(2007/10/02)
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- PRACTICAL ASYMMETRIC SYNTHESIS OF (R)-(-)-PHENYLEPHRINE HYDROCHLORIDE CATALYZED BY (2R,4R)-MCCPM-RHODIUM COMPLEX
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The neutral chiral N-substituted CPM-rhodium complexes were found to be efficient catalysts for asymmetric hydrogenation of 3'-benzyloxy-2-(N-benzyl-N-methyl)aminoacetophenone hydrochloride.A practical asymmetric synthesis of (R)-(-)-phenylephrine hydrochloride catalyzed by newly synthesized (2R,4R)-MCCPM-rhodium complex has been achieved.
- Takeda, Hideo,Tachinami, Takeshi,Aburatani, Masakazu,Takahashi, Hisashi,Morimoto, Toshiaki,Achiwa, Kazuo
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p. 367 - 370
(2007/10/02)
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