- Preparation method of L-penicillamine
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The invention discloses a preparation method of L-penicillamine, which comprises the following steps: protecting sulfydryl and amino in penicillamine by using acetone and ethyl formate to obtain Nformyl isopropyl penicillamine; then, conducting racemization on N-formyl isopropyl-D-apenem by adopting acetic acid or a mixed solution of acetic acid and methylbenzene to acquire N-formyl isopropyl-D and L-apenem; reacting N-formyl isopropyl-D, Lapenem and hydrochloric acid to prepare N-formyl isopropyl-D, L-apenem hydrochloride; dissociating N-formyl isopropyl-D and Lapenem hydrochloride in lower alcohol through organic alkali to obtain a dissociated racemate D and L-apenem; d, reacting the L-Penicillamine with a resolving agent L-tartaric acid to obtain L-Penicillamine. Ltartrate; carrying outsalt hydrolysis on the L-Penicillamine. L-tartrate by using organic alkali to obtain the L-Penicillamine. According to the preparation method disclosed by the invention, the used resolution reagent is low in price, the reaction condition is mild, the product yield is high, and feasibility is provided for industrial mass production of the L-Penicillamine.
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Paragraph 0042-0043; 0047-0048; 0059; 0062
(2021/03/18)
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- NOVEL FLUORESCENT DYES AND USES THEREOF
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The present invention provides fluorescent dyes that are based on firefly luciferin structure. These dyes are optimally excited at shorter wavelengths and have Stokes shift of at least 50 nm. The fluorescent dyes of the invention are useful for preparation of dye-conjugates, which can be used in detection of an analyte in a sample.
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- N-terminal dipeptides of D(-)-penicillamine as sequestration agents for acetaldehyde
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Since acetaldehyde (AcH), a toxic oxidation product of ethanol, may play an etiologic role in the initiation of alcoholic liver disease, we had earlier pioneered the development of β,β-disubstituted-β-mercapto-α-amino acids as AcH-sequestering agents. We now report the synthesis of a series of N-terminal dipeptides of D(-)-penicillamine, prepared from the synthon 3- formyl-2,2,5,5-tetramethylthiazolidine-4S-carboxylic acid (3), a cyclized N- protected derivative of D(-)-penicillamine. These dipeptides were equally or more effective than penicillamine in trapping AcH in a cell-free system. In experiments using a hepatocyte culture system, two of the dipeptides, D- penicillamylglycine (6a) and D-penicillamyl-β-alanine (6d), at 1/20 the molar concentration of ethanol, lowered the concentration of ethanol-derived AcH by 79% and 84%, respectively, at 2 h. The presence of cyanamide (an inhibitor of aldehyde dehydrogenase) in the incubation medium resulted in a 45-fold increase in ethanol-derived AcH; nevertheless, dipeptides 6a and 6c (D-penicillamyl-α-aminoisobutyric acid) were able to reduce this AcH level by approximately one-third.
- Cohen, Jonathan F.,Elberling, James A.,DeMaster, Eugene G.,Lin, Renee C.,Nagasawa, Herbert T.
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p. 1029 - 1033
(2007/10/03)
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