CAS: 120686-17-1; (S)-Tert-Butyl 3-Amino-4-Phenylbutanoate

相似化合物

138165-77-2 26250-87-3 131270-08-1

上下游产品

(S)-3-Benzyloxycarbonylamino-4-phenyl-butyric acid tert-butyl ester (S)-3-benzyloxycarbonylamino-4-phenylbutyric acid tert-butyl 3-amino-4-phenylbut-2-enoate phenylacetic acid(E)-3-((S)-1-tert-Butoxycarbonylmethyl-2-phenyl-ethylcarbamoyl)-4-phenyl-but-3-enoic acid ethyl ester (E)-3-((S)-1-tert-Butoxycarbonylmethyl-2-phenyl-ethylcarbamoyl)-4-phenyl-but-3-enoic acid (S)-3-[(E)-2-(Benzyloxycarbamoyl-methyl)-3-phenyl-acryloylamino]-4-phenyl-butyric acid (S)-3-[(E)-2-(Benzyloxycarbamoyl-methyl)-3-phenyl-acryloylamino]-4-phenyl-butyric acid tert-butyl ester

📜(S)-3-Benzyloxycarbonylamino-4-Phenylbutyric Acid置于palladium On Activated Charcoal 氢气体系中,用 甲醇,苯 用作溶剂,化学反应 5.5H,反应生成(3S)-3-氨基-4-苯基丁酸叔丁酯
参考文献:New Kelatorphan-Related Inhibitors Of Enkephalin Metabolism: Improved Antinociceptive Properties
标题:New Kelatorphan-Related Inhibitors Of Enkephalin Metabolism: Improved Antinociceptive Properties
摘要:In Order To Improve The In Vivo Protection Of Enkephalins From Enzymatic Degradation,A New Series Of Inhibitors Derived From Kelatorphan [honhcoch2Ch(Ch2Ph)Conhch(Ch3)Cooh],The First-Described Complete Inhibitor Of Enkephalin Metabolism,Were Designed By Modification Of The C-Terminal Amino Acid. The Progressive Lengthening Of The Chain Of This Residue Shows That A Beta-Alanine Seems To Be The Best Basic Model For The Conception Of Such Types Of Compounds. On The Other Hand,The Methylation Of The Amide Bond,Which Is Well Accepted By Aminopeptidase N (Ec 3.4.11.2) And Dipeptidylaminopeptidase,Induced A Significant Loss Of Affinity For Neutral Endopeptidase-24.11. Starting From These Data,Compounds Containing A Variously Substituted Beta-Alanine Residue And Corresponding To The General Formula Honhcoch2Ch(Ch2Ph)Conhch(R1)Ch(R2)Cooh Were Synthesized. All These Molecules Inhibit Neutral Endopeptidase-24.11 And Dipeptidylaminopeptidase In The Nanomolar Range,And Those Containing An Aromatic Chain (Compound 7A,R1 = Ch2Ph,R2 = H,And Compound 8A,R1 = Ph,R2 = H) Inhibit The Biologically Relevant Aminopeptidase N,With Ic50'S Around 10(-8) M. Intracerebroventricular Injection In Mice Of These Multienzyme Inhibitors Produced An Efficient And Naloxone-Reversible Analgesic Response (Hot Plate Test): Compounds 7A And 8A Were Shown To Be More Potent Than Kelatorphan In Increasing The Jump Latency Time,In Agreement With Their In Vitro Properties,And These New Compounds Were Found To Increase The Forepaw Lick Latency,A Reflex Considered As A Typical Morphine Response.
Doi:10.1021/jm00127A017

专利信息

专利号:US-8338565-B2
优先权日:2008-08-20
标 题 :Macrocyclic compounds for inhibition of tumor necrosis factor alpha
发明人：LEE JINBO; BOND JULIAN F; TERRETT NICHOLAS; FAVALORO JR FRANK G; WANG DANIEL; BRIGGS TIMOTHY F; SEIGAL BENJAMIN ADAM; SUN WEI-CHUAN; HALE STEPHEN P
权利人:LEE JINBO; BOND JULIAN F; TERRETT NICHOLAS; FAVALORO JR FRANK G; WANG DANIEL; BRIGGS TIMOTHY F; SEIGAL BENJAMIN ADAM; SUN WEI-CHUAN; HALE STEPHEN P; ENSEMBLE THERAPEUTICS CORP
摘要:Disclosed herein are macrocyclic compounds and methods for their synthesis and use. In particular, macrocyclic compounds are disclosed that modulate the activity of tumor necrosis factor alpha and/or are useful in the treatment of medical conditions, such as, rheumatoid arthritis, psoriasis, and asthma.