- Synthesis method of (S)-3-pyrrolidinol hydrochloride
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The invention discloses a synthesis method of (S)-3-pyrrolidinol hydrochloride, which belongs to the field of drug synthesis, and comprises the following steps: dehydrating and amidating L-malic acidand benzylamine as raw materials to obtain (3S)-N-benzyl-3-hydroxypyrrolidine-2,5-diketone, and carrying out one-pot reduction, debenzylation and salification to synthesize (S)-3-pyrrolidinol hydrochloride. The method is short in synthetic route, simple to operate, high in yield, good in product purity and beneficial to industrial production.
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Paragraph 0023; 0026-0028; 0031-0032; 0038-0040
(2020/08/27)
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- Preparation method of (S)-3-hydroxypyrrolidine hydrochloride
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The invention relates to the field of chemistry, particularly a preparation method of a key intermediate (S)-3-hydroxypyrrolidine hydrochloride of darifenacin for treating overactive bladder syndrome and an antihypertensive drug barnidipine. The preparation method comprises the following steps: carrying out Mitsunobu reaction on (R)-1-N-tert-butyloxycarbonyl-3-hydroxypyrrolidine so as to be condensed with acid to obtain an upturned-structure ester, hydrolyzing ester bond under alkaline conditions to obtain (S)-1-N-tert-butyloxycarbonyl-3-hydroxypyrrolidine, and removing Boc protecting groups under acidic conditions, thereby finally obtaining the key intermediate. The method is simple and easy to implement, has the advantages of cheap and accessible raw materials, lower cost and high yield, and has potential production value.
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Paragraph 0031; 0032
(2016/11/09)
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- POLYCYCLIC DERIVATIVES, PREPARATION PROCESS AND PHARMACEUTICAL USE THEREOF
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Disclosed in the present invention are polycyclic derivatives as represented by general formula (I), the preparation method thereof, pharmaceutical compositions containing the derivatives and uses thereof as therapeutic agents, especially the GPR40 agonist and in preparation of drugs for treating diseases such as diabetes and metabolic disorders, etc., wherein each substituent in the general formula (I) has the same definition as in the description.
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Paragraph 0224; 0225
(2015/02/05)
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- POLYCYCLIC DERIVATIVES, PREPARATION METHOD AND MEDICAL USES THEREOF
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Disclosed in the present invention are polycyclic derivatives as represented by general formula (I), the preparation method thereof, pharmaceutical compositions containing the derivatives and uses thereof as therapeutical agents, especially the GPR40 agonist and in preparation of drugs for treating diseases like diabetes and metabolic disorders, etc., wherein each substituent in the general formula (I) has the same definition as in the description.
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Paragraph 0153; 0154
(2014/12/09)
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- Hydrogenation of chiral nitrile on highly ordered mesoporous carbon-supported Pd catalysts
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A highly ordered mesoporous carbon (C-SBA-15 and C-SBA-16) was synthesized by nanocasting method using its corresponding mesoporous silica (SBA-15 and SBA-16) as a template. The obtained porous carbons have high surface areas, large pore volume and a narrow pore size distribution. The N2-adsorption data for C-SBA-15 have provided the BET area of 2029 m2 g-1 and the total pore volume of 1.7 cm3 g-1, and 1637 m2 g-1 and 1.1 cm3 g-1 for C-SBA-16, respectively. The palladium metal impregnated carbon catalysts were employed in the synthesis of (S)-3-pyrrolidinol from chiral (S)-4-chloro-3-hydroxybutyronitrile, and a high yield to (S)-3-pyrrolidinol-salt was obtained by using 1 wt% Pd/C-SBA-16. It was investigated that the well-dispersed Pd metals in the confined mesopores are efficient for the hydrogenation of cyano groups to amine.
- Guo, Xiao-Feng,Kim, Yong-Suk,Kim, Geon-Joong
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experimental part
p. 22 - 27
(2010/11/16)
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- Process for the preparation of 3-pyrrolidinols and intermediates therefor
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3-Pyrrolidinol or its salt is economically produced by cyclizing an aminobutanol derivative of the formula: STR1 wherein R is an alkyl or a substituted or unsubstituted phenyl group, or its salt.
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