CAS: 72599-27-0; (2R,3R,4R,5S)-1-Butyl-2-(Hydroxymethyl)Piperidine-3,4,5-Triol

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CAS号19130-96-2 1-脱氧野尻霉素 | CAS号123-72-8 正丁醛 | CAS号109-65-9 正溴丁烷 | CAS号1538-75-6 特戊酸酐 | CAS号19684-32-3 1,2-O-Isopropyl... | CAS号18549-40-1 单丙酮葡萄糖 | CAS号6564-72-3 四苄基葡萄糖 | CAS号214041-43-7 (2R,3R,4S)-2,3,...

N-Butyl 2,3,4,6-Tetra-O-Benzyl-1,5-Dideoxy-1,5-Imino-D-Glucitol置于氨,Lithium体系中,用 四氢呋喃 作为反应溶剂,化学反应 2.5H,以91%的收率获得产物米格鲁他
参考文献:Synthesis Of 1-Deoxynojirimycin And N-Butyl-1-Deoxynojirimycin
标题:Synthesis Of 1-Deoxynojirimycin And N-Butyl-1-Deoxynojirimycin
摘要:1-Deoxynojirimycin (1) 是一种天然生物碱,具有多种生物活性;例如,其类似物 N-Butyl-1-Deoxynorjirimycin (4) 具有强效的抗 Hiv-1 和 Hiv-2 活性,且无细胞毒性.作为合成具有抗逆转录病毒生物活性的化合物计划的一部分,我们开发了一条以葡萄糖和其他廉价试剂为原料制备 1 和 4 的高效路线.
DOI:10.1055/s-1999-3430

专利信息

专利号:US-9708263-B2
优先权日:2015-04-17
标题:Synthesis of an azasugar and the intermediates thereof
发明人：MALVESTITI ANDREA; BRUNOLDI ENRICO; ATTOLINO EMANUELE
权利人:DIPHARMA FRANCIS SRL
摘要:Process for the preparation of intermediates useful in the synthesis of miglustat and their use in its manufacture.

专利号:WO-2017100796-A1
优先权日:2015-12-11
标 题 :Modulation of globoseries glycosphingolipid synthesis and cancer biomarkers
发明人：WONG CHI-HUEY; HSU TSUI-LING; WU CHUNG-YI; CHEUNG SARAH K C; CHUANG PO-KAI
权利人:SINACA ACAD; WONG CHI-HUEY; HSU TSUI-LING
摘要:The present disclosure relates to methods and compositions which can modulate the globoseries glycosphingolipid synthesis. Particularly, the present disclosure is directed to glycoenzyme inhibitor compound and compositions and methods of use thereof that can modulate the synthesis of globoseries glycosphingolipid SSEA-3/SSEA-4/GloboH in the biosynthetic pathway; particularly, the glycoenzyme inhibitors target the alpha-4GalT; beta- 4GalNAcT-I; or beta-3GalT-V enzymes in the globoseries synthetic pathway. Additionally, the present disclosure is also directed to vaccines, antibodies, and/or immunogenic conjugate compositions targeting the SSEA-3/SSEA-4/GLOBO H associated epitopes (natural and modified) which elicit antibodies and/or binding fragment production useful for modulating the globoseries glycosphingolipid synthesis. Moreover, the present disclosure is also directed to the method of using the compositions described herein for the treatment or detection of hyperproliferative diseases and/or conditions. Furthermore, the instant disclosure also relates to cancer stem cell biomarkers for disgnostic and therapeutic uses.

专利号:US-2017283878-A1
优先权日:2015-12-11
标题:Modulation of globoseries glycosphingolipid synthesis and cancer biomarkers
发明人：WONG CHI-HUEY; WU CHUNG-YI; CHEUNG SARAH K C; CHUANG PO-KAI; HSU TSUI-LING
权利人:ACADEMIA SINICA
摘要:The present disclosure relates to methods and compositions which can modulate the globoseries glycosphingolipid synthesis. Particularly, the present disclosure is directed to glycoenzyme inhibitor compound and compositions and methods of use thereof that can modulate the synthesis of globoseries glycosphingolipid SSEA-3/SSEA-4/GloboH in the biosynthetic pathway; particularly, the glycoenzyme inhibitors target the alpha-4GalT; beta-4GalNAcT-I; or beta-3GalT-V enzymes in the globoseries synthetic pathway. Additionally, the present disclosure is also directed to vaccines, antibodies, and/or immunogenic conjugate compositions targeting the SSEA-3/SSEA-4/GLOBO H associated epitopes (natural and modified) which elicit antibodies and/or binding fragment production useful for modulating the globoseries glycosphingolipid synthesis. Moreover, the present disclosure is also directed to the method of using the compositions described herein for the treatment or detection of hyperproliferative diseases and/or conditions. Furthermore, the instant disclosure also relates to cancer stem cell biomarkers for diagnostic and therapeutic uses.

专利号:US-2004033532-A1
优先权日:2002-08-08
标题 :Use of three-dimensional crystal structure coordinates to design and synthesize domain-selective inhibitors for angiotensin-converting enzyme (ACE)
发明人：EHLERS MARIO R W; HOLMQUIST BARTON
摘要:It has now been discovered that the use of the three-dimensional crystal structure coordinates of angiotensin-converting enzyme (ACE) will enable the design and synthesis, by means of computational chemistry and structure-guided drug design, of inhibitors of ACE that are highly selective and specific for either the N domain or the C domain of the enzyme, for the treatment of diverse diseases. The invention also relates to methods and processes for the structure-guided design and synthesis of dual N- and C-domain ACE inhibitors, and inhibitors that operate by competitive, non-competitive, uncompetitive, and irreversible mechanisms.

专利号:US-5663342-A
优先权日:1994-03-08
标 题 :2-chloro and 2-bromo derivatives of 1,5-iminosugars
发明人：BARTA THOMAS E; MUELLER RICHARD A
权利人:SEARLE & CO
摘要:Novel 2-chloro and 2-bromo derivatives of 1,5-iminosugars are disclosed, especially such derivatives of 1,5-dideoxy-1,5-imino-D-glucitol. These compounds are useful inhibitors of glucosidase enzymes and also are useful as antiviral agents and as intermediates for the synthesis of other enzyme inhibitors and antiviral compounds.

专利号:US-9079856-B2
优先权日:2012-12-06
标 题 :Synthesis of a glycosyltransferase inhibitor
发明人：ATTOLINO EMANUELE; MALVESTITI ANDREA
权利人:ATTOLINO EMANUELE; MALVESTITI ANDREA; DIPHARMA FRANCIS SRL
摘要:Process for the preparation of an iminosugar, and the intermediates thereof, having known activity as a glycosyltransferase inhibitor and used, for example, in the treatment of Gaucher's disease.