CAS: 36692-49-6; Methyl 3,4-Diaminobenzoate

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CAS号67-56-1 甲醇 | CAS号619-05-6 3,4-二氨基苯甲酸 | CAS号22907-68-2 Benzoic acid, 3... | CAS号3987-92-6 4-氨基-3-硝基苯甲酸甲酯 | CAS号1588-83-6 4-氨基-3-硝基苯甲酸 | CAS号528-45-0 3,4-二硝基苯甲酸 | CAS号1539-06-6 4-乙酰氨基-3-硝基苯甲酸 | CAS号64375-41-3 2-硫代-2,3-二氢-1H-... | CAS号132687-01-5 methyl 11-ethyl... | CAS号354793-04-7 2,3-二氧代-1,2,3,4... | CAS号35532-08-2 2-(4-Carboxyphe... | CAS号106429-38-3 2-氨基-1H-苯并咪唑-5-羧酸甲酯 | CAS号106429-57-6 2-氧代-2,3-二氢-1H-... | CAS号7597-41-3 1H-1,3,2-Benzod... | CAS号76391-97-4 2-氨基-1H-苯并咪唑-5-羧酸 | CAS号886497-12-7 2-(3-chlorothio... | CAS号89426-88-0 2-TRIFLUOROMETH...

4-乙酰氨基苯甲酸甲酯置于硫酸,Palladium On Activated Charcoal,氢气,硝酸体系中,用 甲醇,乙酸乙酯 用作溶剂,化学反应 3.0H,反应生成3,4-二氨基苯甲酸甲酯
参考文献:1-芳基-3-(4-甲氧基苄基)脲作为潜在不可逆的糖原合酶激酶3抑制剂:合成和生物学评估.
标题:1-芳基-3-(4-甲氧基苄基)脲作为潜在不可逆的糖原合酶激酶3抑制剂:合成和生物学评估.
摘要:糖原合酶激酶3(gsk-3)因其多因素参与阿尔茨海默氏病的发病机理而闻名.在这项研究中,通过将亲电子战斗部结合到环支架上,合成了拟议的cys199靶向gsk-3β共价抑制剂,合成了1-芳基-3-(4-甲氧基苄基)脲的苯并噻唑和苯并咪唑组.与参考抑制剂ar-A014418(1,Ic50 = 0.072)相比,腈取代的苯并咪唑基尿素2B(ic50 = 0.086+/-0.023 µm)和卤代甲基酮取代的苯并咪唑基尿素9B(ic50 = 0.13+/-0.060 µm)具有较高的gsk-3β抑制活性. +/-0.043).结果表明,对2B和9B作为gsk-3β的潜在共价抑制剂的进一步研究,因为靶向相互作用可能提供改善的激酶选择性.
Doi:10.1016/j.Bmcl.2019.04.049

专利信息

专利号:US-5124478-A
优先权日:1987-12-22
标 题:Acid-labile anchor groups for the synthesis of peptide amides by a solid-phase method
发明人：BREIPOHL GERHARD; KNOLLE JOCHEN; STUEBER WERNER
权利人:HOECHST AG
摘要:The invention relates to new compounds of the formula ##STR1## in which R 1 denotes (C 1 -C 8 )-alkyl, R 2 denotes an amino acid residue which is protected with a urethane protective group which can be eliminated with weak acid or base, or denotes an amino protective group which can be eliminated with weak acid or base, R 3 denotes hydrogen or (C 1 -C 4 )-alkyl, and Y 1 -Y 9 denote identical or different radicals hydrogen, (C 1 -C 4 )-alkyl, (C 1 -C 4 )-alkoxy or --O--(CH 2 ) n --COOH (with n=1 to 6), with one of these radicals being --O--(CH 2 ) n --COOH, or Y 1 , Y 2 and Y 5 -Y 9 denote identical or different radicals hydrogen, (C 1 -C 4 )-alkyl or (C 1 -C 4 )-alkoxy, Y 3 denotes hydrogen or (C 1 -C 8 )-alkoxy and Y 4 denotes --(CH 2 ) n --COOH or --NH--CO--(CH 2 ) n --COOH (with n=1 to 6). n Processes for the preparation thereof and the synthesis of peptide amides by a solid-phase method using these new compounds (spacers) are described.

专利号:US-4922015-A
优先权日:1987-04-08
标 题:Synthesis of peptide amides by means of a solid phase method using acid-labile anchoring groups
发明人：BREIPOHL GERHARD; KNOLLE JOCHEN; STUEBER WERNER
权利人:HOECHST AG
摘要:The invention relates to new compounds of the formula ##STR1## in which R 1 denotes (C 1 -C 8 )-alkyl or optionally substituted (C 6 -C 14 )-aryl, R 2 denotes hydrogen or an amino acid residue which is protected by an amino protective group which can be cleaved off with weak acid or base, R 3 denotes hydrogen or (C 1 -C 4 )-alkyl, and Y 1 -Y 9 denote identical or different radicals hydrogen, (C 1 -C 4 )-alkyl, (C 1 -C 4 )-alkoxy or -O-(CH 2 ) n -COOH (with n=1 to 6), one of these radicals being -O-(CH 2 ) n -COOH. A process for the preparation thereof and the synthesis of peptide amides by means of a solid phase method using these new compounds (spacers) are described.

专利号:US-5565606-A
优先权日:1986-10-21
标 题:Synthesis of peptide aminoalkylamides and peptide hydrazides by the solid-phase method
发明人：BREIPHOL GERHARD; KNOLLE JOCHEN
权利人:HOECHST AG
摘要:The invention relates to compounds of the formula I in which A denotes hydrogen or an amino protective group, B denotes one or more amino acids, X denotes alkylene or aralkylene, Y1, Y2, Y3 and Y4 are identical or different and denote hydrogen, methyl, methoxy or nitro, V denotes hydrogen or a carboxyl protective group, W denotes -[CH2]n- or -O-[CH2]n-, m denotes 0 or 1, n denotes 0 to 6, and p denotes 0 to 5, to a process for their preparation. The compounds of formula I are useful as linkage agents or anchor groups in the solid-phase synthesis of peptide aminoalkylamides and peptide hydrazides.

专利号:US-5554501-A
优先权日:1992-10-29
标题:Biopolymer synthesis using surface activated biaxially oriented polypropylene
发明人：COASSIN PETER J; MATSON ROBERT S; RAMPAL JANG B
权利人:BECKMAN INSTRUMENTS INC
摘要:Disclosed herein are surface activated, organic polymers useful for biopolymer synthesis. Most preferably, aminated biaxially oriented polypropylene is used for the synthesis of oligonucleotides thereto, and these devices are most preferably utilized for genetic analysis of patient samples.

专利号:EP-0721458-B1
优先权日:1993-09-28
标题:Biopolymer synthesis utilizing surface activated, organic polymers
发明人：COASSIN PETER J; MATSON ROBERT S; RAMPAL JANG B
权利人:BECKMAN COULTER INC
摘要:Disclosed herein are surface activated, organic polymers useful for biopolymer synthesis. Most preferably, aminated polypropylene is used for the synthesis of oligonucleotides thereto, and these devices are most preferably utilized for genetic analysis of patient samples.

专利号:US-5990273-A
优先权日:1993-06-29
标 题:Synthesis of cyclic peptides
发明人：ANDERSSON LARS HENRIK HARALD; SKOLDBACK JAN-AKE
权利人:FERRING BV
摘要:A process for preparing and purifying cyclic peptides having disulfide moieties in a two step processing operation including reverse phase chromatography which simplifies synthesis and reduces production costs, yet produces high, quality yield. The improved process is particularly useful for the preparation of vasopressin and oxytocin and their respective derivatives and analogs.