CAS: 55715-03-2; 4-(Bromomethyl)-3-Nitrobenzoic Acid

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CAS号6232-88-8 对溴甲基苯甲酸 | CAS号96-98-0 4-甲基-3-硝基苯甲酸 | CAS号99-94-5 对甲基苯甲酸 | CAS号141884-92-6 4-bromomethyl-3... | CAS号2372-51-2 4-氨基甲基-3-硝基苯甲酸 | CAS号130581-93-0 (2,4,5-trichlor... | CAS号73674-47-2 4-(bromomethyl)... | CAS号82379-38-2 4-羟甲基-3-硝基苯甲酸 | CAS号88089-94-5 4-(溴甲基)-3-硝基苯甲酸甲酯 | CAS号89950-93-6 4-(羟基甲基)-3-硝基苯甲酸甲酯 | CAS号96315-16-1 4-(溴甲基)-3-硝基苯甲酸乙酯 | CAS号62700-58-7 4-(bromomethyl)... | CAS号637338-11-5 4H-1,4-苯并二氮-4,8...

4-甲基-3-硝基苯甲酸置于n-溴代丁二酰亚胺(Nbs),偶氮二异丁腈体系中,用 四氯化碳 作为反应溶剂,化学反应生成 4-溴甲基-3-硝基苯甲酸
参考文献:使用 Cuh 催化高对映选择性合成具有 C3-四元手性中心的吲唑
标题:使用 Cuh 催化高对映选择性合成具有 C3-四元手性中心的吲唑
摘要:C3 取代的 1H-吲唑是许多药物中有用且重要的子结构.与为更亲核的 N1 和 N2 位置开发的反应相比,吲唑直接 C3 官能化的方法相对较少.在此,我们报告了使用 Cuh 催化的 1H-N-(苯甲酰氧基)吲唑的高度 C3 选择性烯丙基化反应.各种具有四元立体中心的 C3-烯丙基 1H-吲唑被高效地制备,具有高水平的对映选择性.进行密度泛函理论 (Dft) 计算以解释吲唑和吲哚亲电试剂之间的反应性差异,后者用于我们之前报道的方法中.计算表明,吲唑烯丙基化反应通过决定对映选择性的六元 Zimmerman-Traxler 型过渡态进行,而不是我们在吲哚烷基化的情况下提出的氧化加成/还原消除序列.该反应的对映选择性受配体-底物空间相互作用和空间排斥两者的控制,这些相互作用涉及六元烯丙基化过渡态中的假多轴取代基.
DOI:10.1021/jacs.0C04286

专利信息

专利号:US-4101721-A
优先权日:1976-12-09
标题 :Solid phase synthesis of protected peptides
发明人：RICH DANIEL H; GURWARA SWEET K
权利人:WISCONSIN ALUMNI RES FOUND
摘要:The invention is addressed to the preparation of 3-nitro-4-bromomethyl benzoic acid, as a new compound from which 3-nitro-4-bromomethyl benzoyl amide polystyrene resin can be prepared for solid synthesis of protected peptide acids and amides and separation thereof without cleavage of acid labile protecting groups or decomposition of aromatic acid groups and from which purified polypeptides can be formed.

专利号:US-4062746-A
优先权日:1975-05-07
标 题 :Solid phase synthesis of protected peptides
发明人：RICH DANIEL H; GURWARA SWEET K
权利人:WISCONSIN ALUMNI RES FOUND
摘要:The invention is addressed to the preparation of 3-nitro-4-bromomethyl benzoic acid, as a new compound from which 3-nitro-4-bromomethyl benzoyl amide polystyrene resin can be prepared for solid synthesis of protected peptide acids and amides and separation thereof without cleavage of acid labile protecting groups or decomposition of aromatic acid groups and from which purified polypeptides can be formed.

专利号:US-6175020-B1
优先权日:1999-04-09
标题 :Spirodiamino acid scaffold for combinatorial synthesis
发明人：DOLLE III ROLAND ELLWOOD; BARDEN MICHAEL C
权利人:PHARMACOPEIA INC
摘要:Azaspirononanes of formula I and their synthesis n are disclosed. The compounds are useful as templates for constructing synthetic receptors and as intermediates in the synthesis of enzyme inhibitors. They are prepared by an intramolecular ylide cycloaddition of a 6-hydrazone of 2,10-undecadienoic acid ester.

专利号:WO-9939207-A1
优先权日:1998-01-29
标题:Acid cleavable phenoxyalkyl linker for combinatorial synthesis
发明人：LI GE; HE ZHEN MIN
权利人:PHARMACOPEIA INC
摘要:A substrate for solid phase synthesis of formula (I) is disclosed. Also disclosed are processes for preparing the substrate and intermediates useful therein. Among the novel intermediates are compounds of formula (II) wherein n is 3-20; R is OH, an activated ester or the residue of a solid support having a plurality of amino functionalities; R1 is lower alkyl or phenyl; R2 is lower alkyl or phenyl; and R3 is lower alkyl, phenyl or lower alkoxy.

专利号:US-6093799-A
优先权日:1998-03-16
标题:Universal linker for combinatorial synthesis
发明人：LI GE; GRIFFITHS SIAN LOUISE; MCDONALD EDWARD; XU LIBO
权利人:PHARMACOPEIA INC
摘要:A substrate for solid phase synthesis of the formula: ##STR1## is disclosed. Also disclosed are processes for preparing the substrate and intermediates useful therein. Among the novel intermediates are compounds of the formula: ##STR2## wherein t is 0 or 1; n is 3-20; R is OH, an activated ester or the residue of a solid support having a plurality of amino functionalities; A is --O-- or --NH-- and Q is hydrogen or a protecting group for an amine or alcohol.

专利号:US-6191277-B1
优先权日:1998-04-29
标 题:Hydroxypropylamide peptidomimetics as inhibitors of aspartyl proteases
发明人：DOLLE III ROLAND ELLWOOD; CAVALLARO CULLEN LEE; HERPIN TIMOTHEE FELIX
权利人:PHARMACOPEIA INC
摘要:Compounds of Formula Iare disclosed as inhibitors having activity against the aspartyl proteases, plasmepsin and cathsepsin D. The compounds are useful for treatment of diseases such as malaria and Alzheimer's disease. In preferred compounds of Formula I, Y is a heterocycle, amide, sulfonamide or carbamate and Z is an acyl or a functionalized acyl. Intermediates in the solid phase synthesis of compounds of Formula I, in which compounds are attached to a solid phase support, are also disclosed.