N-Acetoacetyl-α-L-Aspartyl-L-Phenylalanine Methyl Ester置于盐酸羟胺体系中,用 溶剂黄146 用作溶剂,化学反应生成阿斯巴甜 参考文献:Method And Intermediates For Producing .Alpha.-L-Aspartyl-L-Phenylalanine 标题:Method And Intermediates For Producing .Alpha.-L-Aspartyl-L-Phenylalanine 摘要:这项发明涵盖了一种制备商业甜味剂α-L-天冬氨酸基-L-苯丙氨酸甲酯的方法和中间体.该过程涉及将l-天冬氨酸与二酮乙烯酯反应,形成n-乙酰乙酰-L-天冬氨酸,然后通过与乙酸酐反应将其转化为n-乙酰乙酰-L-天冬氨酸酐.N-乙酰乙酰-L-天冬氨酸酐与l-苯丙氨酸甲酯反应,提供n-乙酰乙酰-α-L-天冬氨酸基-L-苯丙氨酸甲酯,然后通过与盐酸羟胺反应将其转化为α-L-天冬氨酸基-L-苯丙氨酸甲酯.
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:US-2010279334-A1 优先权日:2007-10-31 标题 :Cyclodipeptide synthases (cdss) and their use in the synthesis of linear dipeptides 发明人:SAUGUET LUDOVIC; THAI ROBERT; BELIN PASCAL; LECOQ ALAIN; GENET ROGER; PERNODET JEAN-LUC; GONDRY MURIEL 权利人:KYOWA HAKKO BIO CO LTD; CENTRE NAT RECH SCIENT; UNIV PARIS SUD 11; COMMISSARIAT ENERGIE ATOMIQUE 摘要:Use of CDSs in the synthesis of linear dipeptides, and applications thereof for the in vivo and in vitro synthesis of linear dipeptides, in particular Phe-Leu, Leu-Phe, Phe-Phe, Phe-Tyr, Tyr-Phe, Leu-Leu, Leu-Tyr, Tyr-Leu, Phe-Met, Met-Phe, Leu-Met, Met-Leu, Tyr-Met, Met-Tyr, Met-Met, Tyr-Tyr, Ile-Met, Met-Ile, Leu-Ile, Ile-Leu using the corresponding polynucleotides.
专利号:US-7759520-B2 优先权日:1996-11-27 标 题 :Synthesis of selective androgen receptor modulators 发明人:DALTON JAMES T; MILLER DUANE D; YIN DONGHUA; HE YALI 权利人:UNIV TENNESSEE RES FOUNDATION 摘要:The present invention relates to a synthetic process for the preparation of a novel class of androgen receptor targeting agents (ARTA) which demonstrate androgenic and anabolic activity of a nonsteroidal ligand for the androgen receptor. The agents define a new subclass of compounds which are selective androgen receptor modulators (SARM) which are useful for a) male contraception; b) treatment of a variety of hormone-related conditions, for example conditions associated with Androgen Decline in Aging Male (ADAM), such as fatigue, depression, decreased libido, sexual dysfunction, erectile dysfunction, hypogonadism, osteoporosis, hair loss, anemia, obesity, sarcopenia, osteopenia, osteoporosis, benign prostate hyperplasia, alterations in mood and cognition and prostate cancer; c) treatment of conditions associated with Androgen Decline in Female (ADIF), such as sexual dysfunction, decreased sexual libido, hypogonadism, sarcopenia, osteopenia, osteoporosis, alterations in cognition and mood, depression, anemia, hair loss, obesity, endometriosis, breast cancer, uterine cancer and ovarian cancer; d) treatment and/or prevention of chronic muscular wasting; e) decreasing the incidence of, halting or causing a regression of prostate cancer; f) oral androgen relacement and/or other clinical therpauetic and/or diagnostic areas. The process of the present invention is suitable for large-scale preparation, since all of the steps give rise to highly pure compounds, thus avoiding complicated purification procedures which ultimately lower the yield. Thus the present invention provides methods for the synthesis of non-steroidal agonist compounds, that can be used for industrial large-scale synthesis, and that provide highly pure products in high yield.
专利号:US-6995284-B2 优先权日:2000-08-24 标题 :Synthesis of selective androgen receptor modulators 发明人:DALTON JAMES T; MILLER DUANE D; HE YALI; YIN DONGHUA 权利人:UNIV TENNESSEE RES FOUNDATION 摘要:The present invention relates to a synthetic process for the preparation of a novel class of androgen receptor targeting agents (ARTA) which demonstrate androgenic and anabolic activity of a nonsteroidal ligand for the androgen receptor. The agents define a new subclass of compounds which are selective androgen receptor modulators (SARM) which are useful for a) male contraception; b) treatment of a variety of hormone-related conditions, for example conditions associated with Androgen Decline in Aging Male (ADAM), such as fatigue, depression, decreased libido, sexual dysfunction, erectile dysfunction, hypogonadism, osteoporosis, hair loss, anemia, obesity, sarcopenia, osteopenia, osteoporosis, benign prostate hyperplasia, alterations in mood and cognition and prostate cancer; c) treatment of conditions associated with Androgen Decline in Female (ADIF), such as sexual dysfunction, decreased sexual libido, hypogonadism, sarcopenia, osteopenia, osteoporosis, alterations in cognition and mood, depression, anemia, hair loss, obesity, endometriosis, breast cancer, uterine cancer and ovarian cancer; d) treatment and/or prevention of chronic muscular wasting; e) decreasing the incidence of, halting or causing a regression of prostate cancer; f) oral androgen relacement and/or other clinical therpauetic and/or diagnostic areas. The process of the present invention is suitable for large-scale preparation, since all of the steps give rise to highly pure compounds, thus avoiding complicated purification procedures which ultimately lower the yield. Thus the present invention provides methods for the synthesis of non-steroidal agonist compounds, that can be used for industrial large-scale synthesis, and that provide highly pure products in high yield.
专利号:US-2004249114-A1 优先权日:2001-02-06 标题 :Methods of synthesis of polysuccinimide or polyaspartate by end capping polymerization 发明人:SWIFT GRAHAM; REDLICH GEORGE H; WEHBY JOHN NOLAN 摘要:Disclosed are methods of synthesis of homopolymers or copolymers containing succinimide or aspartate moieties formed in the presence of an end capping initiator. Also disclosed are methods of isolating, compounding, stabilizing and processing the homopolymers and copolymers.
专利号:US-2006211843-A1 优先权日:2001-02-06 标题:Methods of synthesis of poly(succinimide-aspartate) polysuccinimide or polyaspartate by end capping polymerization 发明人:SWIFT GRAHAM; REDLICH GEORGE H 权利人:SWIFT GRAHAM; REDLICH GEORGE H 摘要:Disclosed are methods of synthesis of homopolymers or copolymers containing succinimide or aspartate moieties formed in the presence of an end capping initiator. Also disclosed are methods of isolating, compounding, stabilizing and processing the homopolymers and copolymers.
1: Finamor I, Pavanato MA, Pês T, Ourique G, Saccol E, Schiefelbein S, Llesuy S, Partata W. N-acetylcysteine protects the rat kidney against aspartame-induced oxidative stress. Free Radic Biol Med. 2014 Oct;75 Suppl 1:S30. doi: 10.1016/j.freeradbiomed.2014.10.759. Epub 2014 Dec 10. doi: 10.7555/JBR.28.20120118. Epub 2014 Jan 12. 3: Maillet EL, Cui M, Jiang P, Mezei M, Hecht E, Quijada J, Margolskee RF, Osman R, Max M. Characterization of the Binding Site of Aspartame in the Human Sweet Taste Receptor. Chem Senses. 2015 Oct;40(8):577-86. doi: 10.1093/chemse/bjv045. doi: 10.1016/j.fct.2015.08.021. Epub 2015 Aug 28. Review. doi: 10.1038/sj.bdj.2015.542. doi: 10.1177/0394632015586134. Epub 2015 May 26. doi: 10.1186/s11671-015-0910-7. eCollection 2015.
合成参考文献
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