三甲基硅咪唑,N-三甲基硅基乙酰胺 175.0 °C,20.0 Kpa 条件下,反应生成N,O-双三甲硅基乙酰胺 参考文献:Semi-Continuous Process For Preparing Bis-Silyl Carboxamides 标题:Semi-Continuous Process For Preparing Bis-Silyl Carboxamides 摘要:为了制备半连续的双(硅烷基)羧酰胺,需要将酰胺或其n-三甲基硅基衍生物与硅化剂反应,并同时通过减压蒸馏提取形成的双(硅烷基)羧酰胺.
专利信息
专利号:US-2008032964-A1 优先权日:2006-04-10 标题:Process for the synthesis of azetidinone 发明人:KANSAL VINOD K; AHMAD SUHAIL; MARIAPPAN SHANMUGAVEL; TYAGI BHUPENDRA; PERLMAN NURIT; LE PAIH JACQUES; ZANOTTI-GEROSA ANTONIO 权利人:KANSAL VINOD K; AHMAD SUHAIL; MARIAPPAN SHANMUGAVEL; TYAGI BHUPENDRA; PERLMAN NURIT; LE PAIH JACQUES; ZANOTTI-GEROSA ANTONIO 摘要:Provided are intermediates useful for the synthesis of hydroxyl-alkyl substituted azetidinones, processes of their preparation, and processes for the synthesis of certain hydroxyl-alkyl substituted azetidinones. Also provided are processes for the synthesis of 1-(4-fluorophenyl)-3(R)-[3-(4-fluorophenyl)-3(S)-hydroxypropyl]-4(S)-(4-hydroxyphenyl)-2-azetidinone, or ezetimibe.
专利号:WO-2022256490-A9 优先权日:2021-06-03 标题:Improved synthesis of phosphoramidates for the treatment of hepatitis b virus 发明人:LOCKWOOD MARK 权利人:ANTIOS THERAPEUTICS INC 摘要:The synthesis of phosphoramidate prodrugs useful in the treatment of viral infections is disclosed. Specifically, an improved synthesis of phosphoramidate nucleotides useful in the treatment of Hepatitis B virus is disclosed.
专利号:US-2009131688-A1 优先权日:2007-11-21 标 题 :Method for the synthesis of 4-benzofuran-carboxylic acid 发明人:BURGOS ALAIN; MARUANI MARTINE; PERRIN FLORENCE; FREIN STEPHANE 权利人:ZACH SYSTEM 摘要:The invention concerns a novel method for synthesis of 4-benzofuran-carboxylic acid or alkyl ester thereof. n This method is characterized in that a reaction for aromatization of a compound of formula (II) is performed for the synthesis of the compound of formula (I), according to the scheme A2 below: n n n n n n n n n n wherein R independently represents hydrogen or a linear or branched C 1 - 15 alkyl group. n With the invention, it is possible to industrially synthesize 4-benzofuran-carboxylic acid or alkyl ester thereof with good yield and very good purity.
专利号:US-6639059-B1 优先权日:1999-03-24 标 题 :Synthesis of [2.2.1]bicyclo nucleosides 发明人:KOCHKINE ALEXEI; FENSHOLDT JEF; PFUNDHELLER HENRIK M 权利人:EXIQON AS 摘要:A synthesis of [2.2.1]bicyclo nucleosides which is shorter and provides higher overall yields proceeds via the key intermediate of the general formula III, wherein R4 and R5 are, for instance, sulfonates and R7 is, for instance, a halogen or an acetate. From compounds of the general formula II, such as 3-O-aryl-4-C-hydroxymethyl-1,2-O-isopropylidene-alpha-D-ribofuranose, intermediates of the general formula III are suitable for coupling with silylated nucleobases. Upon one-pot base-induced ring-closure and desulfonation of the formed [2.2.1]bicyclo nucleoside, a short route to each the LNA (Locked Nucleic Acid) derivatives of adenosine, cytosine, uridine, thymidine and guanidine is demonstrated. The use of the 5'-sulfonated ring-closed intermediate also allows for synthesis of 5'-amino- and thio-LNAs.
专利号:US-6734291-B2 优先权日:1999-03-24 标题:Synthesis of [2.2.1]bicyclo nucleosides 发明人:KOCHKINE ALEXEI; FENSHOLDT JEF; PFUNDHELLER HENRIK M 权利人:EXIQON AS 摘要:A synthesis of [2.2.1]bicyclo nucleosides which is shorter and provides higher overall yields proceeds via the key intermediate of the general formula III, wherein R4 and R5 are, for instance, sulfonates and R7 is, for instance, a halogen or an acetate. From compounds of the general formula II, such as 3-O-aryl-4-C-hydroxymethyl-1,2-O-isopropylidene-alpha-D-ribofuranose, intermediates of the general formula III are suitable for coupling with silylated nucleobases. Upon one-pot base-induced ring-closure and desulfonation of the formed [2.2.1]bicyclo nucleoside, a short route to each the LNA (Locked Nucleic Acid) derivatives of adenosine, cytosine, uridine, thymidine and guanidine is demonstrated. The use of the 5'-sulfonated ring-closed intermediate also allows for synthesis of 5'-amino- and thio-LNAs
专利号:US-2024383940-A1 优先权日:2021-03-31 标题 :Synthesis of trinucleotide and tetranucleotide caps for mrna production 发明人:ENDO ATSUSHI 权利人:MODERNA TX INC 摘要:Provided herein are methods of making trinucleotides and tetranucleotides for use as 5′ mRNA caps. The methods utilize a novel “top-downâ€? strategy and provide for synthesis of oligonucleotides with higher yields and increased efficiency compared to traditional methods. A key step of the methods disclosed, herein can also be adapted to utilize a “one-potâ€? approach, resulting in an increase in the yield of the final oligonucleotide product.
[参考文献]: Chad J Roy, Et Al. Thermostable Ricin Vaccine Protects Rhesus Macaques Against Aerosolized Ricin: Epitope-Specific Neutralizing Antibodies Correlate With Protection. Proc Natl Acad Sci U S A. 2015 Mar 24;112(12):3782-7. [参考文献]: Colleen E Dugan, Et Al. Multiplexed Microfluidic Enzyme Assays For Simultaneous Detection Of Lipolysis Products From Adipocytes. Anal Bioanal Chem. 2014 Aug;406(20):4851-9. [参考文献]: Elisabetta Moratti, Et Al. Identification Of Protein Tyrosine Phosphatase Receptor Gamma Extracellular Domain (Sptprg) As A Natural Soluble Protein In Plasma. Plos One. 2015 Mar 16;10(3):E0119110. [参考文献]: Ghazal Fadaeian, Et Al. Targeted Delivery Of 5-Fluorouracil With Monoclonal Antibody Modified Bovine Serum Albumin Nanoparticles. Iran J Pharm Res. 2015 Spring;14(2):395-405. [参考文献]: Peter Podolec, Et Al. Direct Silylation Of Trypanosoma Brucei Metabolites In Aqueous Samples And Their Gc-Ms/ms Analysis. J Chromatogr B Analyt Technol Biomed Life Sci. 2014 Sep 15:967:134-8.
合成参考文献
摘要:Silva, V. L. M.; Pinto, D. C. G. A.; Santos, C. M. M.; Rocha, D. H. A., Science of Synthesis Knowledge Updates, (2022) 3, 328. 摘要:Kleemann A., Kutscher B., Reichert D., Bossart M., Pharmaceutical Substances, Thieme [Online], Stuttgart, (2025).