CAS: 59787-61-0; (3S,6S,9S,12R,15S,18S,21S,24S,30S,33S)-33-((1R,2R,E)-1-Hydroxy-2-Methylhex-4-En-1-yl)-30-((R)-1-Hydroxyethyl)-6,9,18,24-Tetraisobutyl-3,21-Diisopropyl-1,4,7,10,12,15,19,25,28-Nonamethyl-1,4,7,10,13,16,19,22,25,28,31-Undecaazacyclotritriacontan-2,5,8,11,14,17,20,23,26,29,32-Undecaone

上下游产品

Cyclosporin A 79217-60-0
双氢环孢菌素c 24-Tert-Butyl-30-(1-Hydroxyethyl)-33-(1-Hydroxy-2-Methylhexyl)-1,4,7,10,12,15,19,25,28-Nonamethyl-6,9,18-Tris(2-Methylpropyl)-3,21-Di(Propan-2-yl)-1,4,7,10,13,16,19,22,25,28,31-Undecazacyclotritriacontane-2,5,8,11,14,17,20,23,26,29,32-Undecone 63556-15-0

C70H117N11O14置于盐酸体系中,用 四氢呋喃 作为反应溶剂,化学反应 300.0H,以100%的收率获得产物环孢菌素 C
参考文献:Pseudoprolines (Pro) In Drug Design: Direct Insertion Of Pro Systems Into Cyclosporin C
标题:Pseudoprolines (Pro) In Drug Design: Direct Insertion Of Pro Systems Into Cyclosporin C
摘要:The Insertion Of Acetals That Exhibit Variable Structural Features Into Complex Peptides Such As Cyclosporin C (Csc) Results In Oxazolidine Derivatives (Pseudoprolines,Psi Pro) Of Tailored Physico-Chemical And Biological Properties. N,O-Acetalation Of The 2-Threonine Hydroxyl Group And The Preceding Amide Nitrogen Of Csc Is Achieved By Treating The Molecule With A Number Of Both Arylated And Non-Arylated Dimethyl Acetals. The Psi Pro-Containing Csc Derivatives Exhibit Enhanced Conformational Backbone Rigidity,As Suggested By Analytical HPLC,NMR Spectroscopy And By Kinetic Measurements On Binding With Their Receptor Protein Cyclophilin A (Cypa) That Were Not Time-Dependent. Ic50 Values For Calf-Thymus Cypa Were Obtained By Kinetic Evaluation Of Its Cis--> Trans Isomerase Activity. The Choice Of The Pam-Substituted Aryl Dimethyl Acetals Allows The Inhibitory Properties Of The Corresponding Derivatives To Be Modulated To Either Prodrugs Or Moderately Strongly Binding Cyclosporin C Derivatives.
DOI:10.1002/1521-3765(20001201)6:23<4358::Aid-Chem4358>3.0.Co;2-W

专利信息

专利号:US-4396542-A
优先权日:1980-02-14
标 题 :Method for the total synthesis of cyclosporins, novel cyclosporins and novel intermediates and methods for their production
发明人：WENGER ROLAND
权利人:SANDOZ LTD
摘要:A method for the total synthesis of cyclosporins, in particular Cyclosporin A, cyclosporins produced in accordance with the method of the invention and novel intermediates, in particular novel [1S, 2R, 3R]- and [1R, 2S, 3S]-1-nitrilo-1-carbonyl-3-methyl-2-oxy-heptanes and -hept-5-enes, employed in the method of the invention.

专利号:US-4554351-A
优先权日:1980-02-14
标 题:Method for the total synthesis of cyclosporins, novel cyclosporins and novel intermediates and methods for their production
发明人：WENGER ROLAND
权利人:SANDOZ LTD
摘要:A method for the total synthesis of cyclosporins, in particular Cyclosporin A, cyclosporins produced in accordance with the method of the invention and novel intermediates, in particular novel [1S, 2R, 3R]- and [1R, 2S, 3S]-1-nitrilo-1-carbonyl-3-methyl-2-oxy-heptanes and -hept-5-enes, employed in the method of the invention.

专利号:US-5214130-A
优先权日:1990-02-27
标题 :Synthesis of novel immunosuppressive cyclosporin analogs with modified amino acids at position-8
发明人：PATCHETT ARTHUR A; TAUB DAVID; GOEGELMAN ROBERT T
权利人:MERCK & CO INC
摘要:New immunosuppressive cyclosporin analogs are disclosed consisting of [dehydro-Ala]8 cyclosporins and derived therefrom cyclosporins having a sulfur containing amino acid at position-8.

专利号:US-7910327-B2
优先权日:2004-07-14
标题:Recombinant alpha-fetoprotein and method of preparing
发明人：BENEVOLENSKY SERGEI VLADIMIROVICH; MARCHENKO ALEXEI NIKOLAEVICH; KOZLOV DMITRY GEORGIEVICH; ZATSEPIN SERGEI SERGEEVICH; SHINGAROVA LYUDMILA NIKOLAEVNA; DUDICH IGOR VYACHESLAVOVICH; SEMENKOVA LIDIYA NIKOLAEVNA; DUDICH DMITRY IGOREVICH; TATULOV EDUARD BORISOVICH; DUDICH ELENA IVANOVNA
权利人:BENEVOLENSKY SERGEI VLADIMIROVICH; MARCHENKO ALEXEI NIKOLAEVICH; KOZLOV DMITRY GEORGIEVICH; ZATSEPIN SERGEI SERGEEVICH; SHINGAROVA LYUDMILA NIKOLAEVNA; DUDICH IGOR VYACHESLAVOVICH; SEMENKOVA LIDIYA NIKOLAEVNA; DUDICH DMITRY IGOREVICH; TATULOV EDUARD BORISOVICH; DUDICH ELENA IVANOVNA
摘要:The invention relates to the microbiological and medical industry, genetic engineering, biotechnology. A Saccharomyces cerevisiae yeast strain was obtained on the basis of constructing a recombinant plasmid DNA comprising a structural gene of a human alpha-fetoprotein (AFP) under the control of a regulatory promoter, providing the synthesis and production of AFP in a secreted soluble form, this AFP having activity identical or similar to the activity of a human AFP. The obtained recombinant AFP may be used as an active substance for the preparation of therapeutic agents for use in oncology, immunotherapy, cosmetology and also for the diagnosis of cancer and embryonic pathologies.

专利号:EP-0034567-B1
优先权日:1980-02-14
标 题 :A method for the total synthesis of cyclosporins and novel cyclosporins

专利号:EP-0098457-B1
优先权日:1980-02-14
标 题:(1s,2r,3r)- and (1r,2s,3s)-nitrilo-1-carbonyl-3-methyl-2-oxy-heptanes and -hept-5-enes useful in the total synthesis of cyclosporins and processes for their production