CAS: 41153-30-4; Boc-Phe(4-F)-Oh

相似化合物

169243-86-1 177966-64-2 18125-46-7

上下游产品

CAS号24424-99-5 二碳酸二叔丁酯 | CAS号51-65-0 4-氟-DL-苯丙氨酸 | CAS号1132-68-9 L-4-氟苯丙氨酸 | CAS号58632-95-4 2-(叔-丁氧基碳酰胺)-2-苯乙腈 | CAS号834888-50-5 (R)-1-(2-氨基-3-(...

二碳酸二叔丁酯置于三乙胺,Lithium Hydroxide体系中,用 四氢呋喃,二氯甲烷,水 作为反应溶剂,化学反应 4.0H,反应生成 Boc-L-4-氟苯丙氨酸
参考文献:磷酸盐和氨基酸酯前药的设计,合成和药代动力学评估,可改善hiv-1蛋白酶抑制剂阿扎那韦的口服生物利用度.
标题:磷酸盐和氨基酸酯前药的设计,合成和药代动力学评估,可改善hiv-1蛋白酶抑制剂阿扎那韦的口服生物利用度.
摘要:制备了hiv-1蛋白酶抑制剂(pi)阿扎那韦(1)的磷酸盐和氨基酸前药,并进行了评估,以解决溶解度和吸收限制的问题.尽管磷酸盐前药未能在大鼠中释放1,但亚甲基间隔基的引入促进了前药的活化,但母体暴露量低于直接给药1后的水平.val氨基酸和val-Val二肽赋予母体较低的血浆暴露,尽管前药的暴露量很高,反映了非常好的吸收.筛选其他氨基酸导致鉴定出1-Phe酯,该酯可改善暴露1并降低循环前药的水平.
DOI:10.1021/acs.Jmedchem.9B00002

专利信息

专利号:WO-9834113-A1
优先权日:1997-02-04
标题 :Combinatorial libraries of bicyclic guanidine derivatives and compounds therein
发明人：OSTRESH JOHN M; MEYER JEAN-PHILIPPE; DOOLEY COLETTE T; HOUGHTEN RICHARD A; BLONDELLE SYLVIE E; SCHONER CHRISTA C
权利人:TREGA BIOSCIENCES INC
摘要:The invention provides a rapid approach for combinatorial synthesis and screening of combinatorial libraries of bicyclic guanidine compounds. The present invention further provides the compounds made by the combinatorial synthesis and individually as well as methods of using the same.

专利号:US-6359144-B1
优先权日:1997-02-04
标 题 :Combinatorial libraries of bicyclic guanidine derivatives and compounds therein
发明人：OSTRESH JOHN M; MEYER JEAN-PHILIPPE; DOOLEY COLETTE T; BLONDELLE SYLVIE E; SCHONER CHRISTA C; HOUGHTEN RICHARD A
权利人:LION BIOSCIENCE AG
摘要:The invention provides a rapid approach for combinatorial synthesis and screening of combinatorial libraries of bicyclic guanidine compounds. The present invention further provides the compounds made by the combinatorial synthesis and individually as well as methods of using the same.

专利号:US-6872745-B2
优先权日:2000-04-14
标 题 :Antipicornaviral compounds and compositions, their pharmaceutical uses, and materials for their synthesis
发明人：JOHNSON JR THEODORE O; HUA YE; LUU HIEP T; DRAGOVICH PETER S
权利人:AGOURON PHARMA
摘要:Compounds of the formula: n n nwhere the formula variables are as defined in the disclosure, advantageously inhibit or block the biological activity of the picornaviral 3C protease. These compounds, as well as pharmaceutical compositions containing these compounds, are useful for treating patients or hosts infected with one or more picornaviruses, such as RVP. Intermediates and synthetic methods for preparing such compounds are also described.

专利号:RU-2067585-C1
优先权日:1991-09-12
标 题 :Derivatives of 5-amino-4-hydroxyhexanoic acid and a method of their synthesis

专利号:CN-102241737-B
优先权日:2011-04-06
标 题 :Endomorphin-1 analogs and their synthesis and application in the preparation of analgesic drugs

专利号:CN-102241737-A
优先权日:2011-04-06
标 题:Endomorphin-1 analogs and their synthesis and application in the preparation of analgesic drugs