1123-19-9Relevant articles and documents
Pentazocine prodrug as well as preparation method and application thereof
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Paragraph 0040-0043; 0078-0080; 0082-0084; 0111-0112, (2020/07/15)
The invention discloses a pentazocine prodrug shown as a formula (I), a preparation method thereof and medical application of a pharmaceutical preparation containing the pentazocine prodrug, wherein Ris hydrogen or deuterium. The water solubility of the prodrug compound is improved by 20 times or above at room temperature, the prodrug compound is chemically stable, the onset time is delayed, thedrug effect is prolonged, meanwhile, the same parent drug blood concentration is generated at a low dosage, and the prodrug compound has a wide clinical application prospect.
A new 2H-azirin-3-amine as a synthon for 2-methylaspartate
Brun, Kathrin A.,Heimgartner, Heinz
, p. 2951 - 2959 (2007/10/03)
The synthesis of a novel 2,2-disubstituted 2H-azirin-3-amine 3a as a building block for racemic Asp(2Me) is described. This synthon contains an ester group in the side chain. The reaction of 3a with thiobenzoic acid and the amino acid Z-Val-OH yielded the racemic monothiodiamide 10a and the dipeptide 11 as a mixture of diastereoisomers, respectively (Scheme 2). In 11, each of the protecting groups was removed selectively (Scheme 3). First attempts toward the preparation of enantiomerically pure synthons for Asp(2Me) with a chiral auxiliary group in the side chain are described. Synthons 3b with a 1-(naphthalen-1-yl)ethyl ester group and 3c with a menthyl ester group were prepared and reacted with thiobenzoic acid to form monothiodiamides 10b and 10c (Scheme 2). However, the diastereoisomers of the synthons 3b and 3c could not be separated by chromatography.
Selective Alkylation of β-Ketoester Enolates using O-Methyl Aminosulfoxonium salts; the First Example of C-alkylation using Sulfoxonium Salt Electrophiles
Pickersgill, I. Fraser,Marchington, Allan P.,Rayner, Christopher M.
, p. 2597 - 2598 (2007/10/02)
The alkylation of β-ketoester enolates with O-methyl aminosulfoxonium tetraphenylborate salts is reported; good to excellent selectivity for C- vs.O-alkylation is observed, and is found to be dependent on the nature of the β-ketoester, solvent, metal counterion and aminosulfoxonium salt.
