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2-甲基萘置于cytochrome P450 Monooxygenase Enzyme Cyp101B1体系中,化学反应生成2-萘甲醇
参考文献:取代的芳族烃的选择性氧化和脱开的观察通过由cyp101B1系统萘氧化期间氧化还原循环†
标题:取代的芳族烃的选择性氧化和脱开的观察通过由cyp101B1系统萘氧化期间氧化还原循环†
摘要:细胞色素p450单加氧酶cyp101B1,来自novosphingobium芳烃dsm12444有效且选择性地氧化了各种萘和联苯衍生物.甲基取代的萘是比乙基萘和萘本身更好的底物.用2-甲基萘获得单取代烷基萘的最高产物形成活性.烷基萘的氧化对苄基甲基或次甲基ch键具有区域选择性.来自1-和2-乙基萘氧化的产物是高度对映体选择性的,并且明显过量地产生了单个立体异构体.与1-和2-甲基萘相比,双取代的底物2,7-二甲基萘具有更高的产物形成活性.甲基取代的联苯也是比联苯更好的底物,并且具有与1-甲基萘相似的生物催化参数.Cyp101B1催化的2-和3-甲基联苯的氧化对甲基ch键具有选择性.例外的是4-甲基联苯的周转量,它以4'-(4-甲基苯基)苯酚为主要产物(占70%),其余部分由4-联苯甲醇构成.药物分子双氯芬酸也被cyp101B1区域选择性氧化为4'-羟基双氯芬酸.带有萘的cyp101B1系统
Doi:10.1039/c7Cy00088J

专利信息

专利号:WO-03031376-A1
优先权日:2001-10-12
标 题 :Solid phase synthesis of substituted 1,5-benzodiazepine-2-one and 1,5-benzothiazepine-2-one
发明人：MORTON GEORGE C; SALVINO JOSEPH M; LABAUDINIERE RICHARD F; HERPIN TIMOTHY F
权利人:AVENTIS PHARMA INC; MORTON GEORGE C; SALVINO JOSEPH M; LABAUDINIERE RICHARD F; HERPIN TIMOTHY F
摘要:A solid phase synthetic method for making substituted 1,5-benzodiazepine-2-one or 1,5-benzothiazepine-2-one. The method is useful for synthesis of large numbers of compounds through automated parallel synthesis or combinatorial library generation and is thus important to rapid discovery or new therapeutic agents containing the base structure of 1,5-benzodiazepine-2-one or 1,5-benzothiazepine-2-one.

专利号:US-6022963-A
优先权日:1995-12-15
标 题:Synthesis of oligonucleotide arrays using photocleavable protecting groups
发明人：MCGALL GLENN H; NAM NGO QUOC
权利人:AFFYMETRIX INC
摘要:Novel compounds are provided which are useful as linking groups in chemical synthesis, preferably in the solid phase synthesis of oligonucleotides and polypeptides. These compounds are generally photolabile and comprise protecting groups which can be removed by photolysis to unmask a reactive group. The protecting group has the general formula Ar-C(R1)(R2)-O-C(O)- wherein: Ar is an optionally substituted fused polycyclic aryl or heteroaromatic group or a vinylogous derivative thereof; R1 and R2 are independently H, optionally substituted alkyl, alkenyl or alkynyl, optionally substituted aryl or optionally substituted heteroaromatic, or a vinylogous derivative of the foregoing; and X is a leaving group, a chemical fragment linked to Ar-C(R1)(R2)-O-C(O)- via a heteroatom, or a solid support; provided that when Ar is 1-pyrenyl and R1=R2=H, X is not linked to Ar-C(R1)(R2)-O-C(O)- via a nitrogen atom. Preferred embodiments are those in which Ar is a fused polycyclic aromatic hydrocarbon and in which the substituents on Ar, R1 and R2 are electron donating groups. A particularly preferred protecting group is the 'PYMOC' protecting group, pyrenylmethyloxycarbonyl, where Ar=pyrenyl and R1=R2=H. Also provided is a method of forming, from component molecules, a plurality of compounds on a support, each compound occupying a separate predefined region of the support, using the protected compounds described above.

专利号:US-7138526-B1
优先权日:1999-06-15
标 题 :Solid phase synthesis of n,n-disubstituted diazacycloalkylcarboxy derivatives
发明人：HERPIN TIMOTHY F; MORTON GEORGE C; SALVINO JOSEPH M
权利人:AVENTIS PHARMA INC
摘要:A method for the solid phase synthesis of N,N-disubstituted diazacycloalkylcarboxy derivatives of general formula (I) and (II) is claimed. Examples include piperazine-2-carboxamide. The method is applicable to the synthesis or large combinatorial libraries

专利号:US-6127515-A
优先权日:1997-11-18
标 题:Functionalized resin for the synthesis of amides and peptides
发明人：MANFRE FRANCO; VANASSE BENOIT J; LABAUDINIERE RICHARD F; MORTON GEORGE C
权利人:AVENTIS PHARM PROD INC
摘要:This invention is directed to a functionalized amino resin of formula ##STR1## wherein S is a solid support; R is H or alkyl; A is ##STR2## Y is OH or OCOR 1 ; and R 1 is aliphatic or aromatic which is useful for the solid phase synthesis of amides, peptides and hydroxamic acids.

专利号:US-6133409-A
优先权日:1996-12-19
标 题:Process for the solid phase synthesis of aldehyde, ketone, oxime, amine, hydroxamic acid and αβ-unsaturated carboxylic acid and aldehyde compounds
发明人：SALVINO JOSEPH M; MORTON GEORGE C; MASON HELEN J; LABAUDINIERE RICHARD F
权利人:AVENTIS PHARM PROD INC
摘要:This invention is directed to a process for the solid phase synthesis of aldehyde, ketone, oxime, amine, hydroxamic acid and alpha , beta -unsaturated carboxylic acid and aldehyde compounds and to polymeric hydroxylamine resin compounds useful therefor.

专利号:US-6710208-B2
优先权日:1996-12-19
标题 :Process for the solid phase synthesis of aldehyde, ketone, oxime, amine, hydroxamic acid and α,β-unsaturated carboxylic acid and aldehyde compounds
发明人：SALVINO JOSEPH M; MORTON GEORGE C; MASON HELEN J; LABAUDINIERE RICHARD F
权利人:AVENTIS PHARMA INC
摘要:This invention is directed to a process for the solid phase synthesis of aldehyde, ketone, oxime, amine, hydroxamic acid and α,β-unsaturated carboxylic acid and aldehyde compounds and to polymeric hydroxylamine resin compounds useful therefor.