CAS: 123-08-0; 4-Hydroxybenzaldehyde

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767-00-0 623-05-2 284474-52-8

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对羟基苯乙酸置于咪唑,Sodium Periodate,{mn(III)[5,10,15,20-Tetrakis(4-H2N-Ph)Porphyrin]}Polystyrene体系中,用 乙腈 用作溶剂,化学反应 2.5H,以90%的收率获得对羟基苯甲醛
参考文献:负载型锰(III)卟啉催化高碘酸钠对羧酸进行高效氧化脱羧.
标题:负载型锰(III)卟啉催化高碘酸钠对羧酸进行高效氧化脱羧.
摘要:研究了负载型锰(III)卟啉对羧酸的氧化脱羧作用.在使用交联的氯甲基化聚苯乙烯[mn(h(2)ntpp)-Cmp]负载的5,10,15,20-四(4-氨基苯基)卟啉锰(III)氯化物作为催化剂的化学系统中,羧酸被转化通过与高碘酸钠的氧化脱羧反应生成相应的羰基化合物.
Doi:10.1016/s0960-894X(03)00749-2

专利信息

专利号:WO-2021014395-A1
优先权日:2019-07-24
标题:Process for the synthesis of deuterated capsaicin, capsaicinoids and synthetic capsaicin analogs
发明人：ORUGANTI SRINIVAS; AMRUTAPU SRAVANTH KUMAR; SAMPATH MAGESH; SEN SAIKAT
权利人:DR REDDY’S INST OF LIFE SCIENCES
摘要:The present application provides novel processes for the synthesis of deuterated intermediates of capsaicinoids, particularly II, III, IV and V of capsaicinoids, relating to pharmaceutical applications. The invention also provides novel intermediates of compounds of formula IX, XIV, XV, XVI, XVII, XVIII, XX and XXI utilized in the process of making deuterated capsaicin II, III, IV and V.

专利号:US-7589170-B1
优先权日:1998-09-25
标题 :Synthesis of cyclic peptides
发明人：SMYTHE MARK LESLIE; MEUTERMANS WIM DENIS FRANS; BOURNE GREGORY THOMAS; MCGEARY ROSS PETER
权利人:UNIV QUEENSLAND
摘要:This invention relates to methods for preparing cyclic peptides and peptidomimetic compounds in solution and bound to solid supports, and to cyclic peptide or peptidomimetic libraries for use in drug screening programs. In particular, the invention relates to a generic strategy for synthesis of cyclic peptides or peptidomimetics that enables the efficient synthesis under mild conditions of a wide variety of desired compounds. Two approaches were evaluated for their improvements in solution and solid phase synthesis of small cyclic peptides: positioning reversible N-amide substituents in the sequence; and applying native ligation chemistry in an intramolecular sense. Systematic investigation of the effects of preorganising peptides prior to cyclisation by using peptide cyclisation auxiliaries, and developing new linkers and peptide cyclisation auxiliaries to aid cyclic peptide synthesis gives surprising improvements in both yields and purity of products compared to the prior art methods. The combination of these technologies provides a powerful generic approach for the solution and solid phase synthesis of small cyclic peptides. The ring contraction and N-amide substitution technology of the invention provide improved methods for the synthesis of cyclic peptides and peptidomimetics. When used in conjunction with linker strategies, this combination provides solid-phase avenues to cyclic peptides and peptidomimetics.

专利号:US-6251689-B1
优先权日:1998-05-14
标 题:Methods for the solid phase synthesis of combinatorial libraries of benzimidazoles benzoxazoles benzothiazoles and derivatives thereof
发明人：LABORDE EDGARDO; MATSUMOTO YUKIHARU
权利人:TELIK INC
摘要:The present invention provides an efficient and versatile method for the synthesis and screening of combinatorial libraries of benzimidazoles, benzoxazoles, benzothiazoles, and derivatives thereof. In order to expedite the synthesis of large arrays of compounds possessing these core structures, a general methodology for solid phase synthesis of these derivatives is provided. Arrays of benzimidazoles, benzoxazoles, benzothiazoles, and derivatives thereof useful as peptidomimetics and for the identification of agents having antifungal, antiviral, antimicrobial, anticoagulant, and antiulcer activity, or use in the treatment of inflammation, hypertension, cancer, and other conditions can be prepared by this method.

专利号:US-5861532-A
优先权日:1997-03-04
标 题:Solid-phase synthesis of N-alkyl amides
发明人：BROWN EDWARD G; NUSS JOHN M
权利人:CHIRON CORP
摘要:Methods for solid phase synthesis of N-alkyl amides comprise reductive amination of carbonyl compounds using a reducing agent and an amine-containing linker bound to a solid support. The methods afford high yields of linker-bound, monoalkylated amines, and subsequent coupling with acid derivatives provide derivatized N-substituted amides in excellent yields after cleavage from the solid-phase. Compositions useful in solid phase synthesis are also described.

专利号:US-11512303-B2
优先权日:2017-05-27
标 题 :Engineered polypeptides and their applications in the synthesis of beta-hydroxy-alpha-amino acids
发明人：CHEN HAIBIN; BONG YONG KOY; XU QING; ZHOU AMENG; SHEN TIANRAN; YANG JIADONG; YANG ZHUHONG
权利人:ENZYMASTER NINGBO BIO ENG CO LTD
摘要:The present invention provides engineered polypeptides that are useful for the asymmetric synthesis of β-hydroxy-α-amino acids under industrial-relevant conditions. The engineered polypeptides disclosed in this invention were developed through directed evolution based on the ability of catalytic synthesis of (2S, 3R)-2-amino-3-hydroxy-3-(4-nitrophenyl) propanoic acid. The present disclosure also provides polynucleotides encoding engineered polypeptides, host cells capable of expressing engineered polypeptides, and methods of producing β-hydroxy-α-amino acids using engineered polypeptides. Compared to other processes of preparation, the use of the engineered polypeptides of the present invention for the preparation of β-hydroxy-α-amino acids results in high purity of the desired stereoisomers, mild reaction conditions, low pollution and low energy consumption. So, it has good industrial application prospects.

专利号:US-5877278-A
优先权日:1992-09-24
标题:Synthesis of N-substituted oligomers
发明人：ZUCKERMANN RONALD N; GOFF DANE A; NG SIMON; SPEAR KERRY; SCOTT BARBARA O; SIGMUND AARON C; GOLDSMITH RICHARD A; MARLOWE CHARLES K; PEI YAZHONG; RICHTER LUTZ; SIMON REYNA
权利人:CHIRON CORP
摘要:A solid-phase method for the synthesis of N-substituted oligomers, such as poly (N-substituted glycines) (referred to herein as poly NSGs) is used to obtain oligomers, such as poly NSGs of potential therapeutic interest which poly NSGs can have a wide variety of side-chain substituents. Each N-substituted glycine monomer is assembled from two 'sub-monomers' directly on the solid support. Each cycle of monomer addition consists of two steps: (1) acylation of a secondary amine bound to the support with an acylating agent comprising a leaving group capable of nucleophilic displacement by -NH2, such as a haloacetic acid, and (2) introduction of the side-chain by nucleophilic displacement of the leaving group, such as halogen (as a solid support-bound alpha -haloacetamide) with a sufficient amount of a second sub-monomer comprising an -NH2 group, such as a primary amine, alkoxyamine, semicarbazide, acyl hydrazide, carbazate or the like. Repetition of the two step cycle of acylation and displacement gives the desired oligomers. The efficient synthesis of a wide variety of oligomeric NSGs using automated synthesis technology of the present method makes these oligomers attractive candidates for the generation and rapid screening of diverse peptidomimetic libraries. The oligomers of the invention, such as N-substituted glycines (i.e. poly NSGs) disclosed here provide a new class of peptide-like compounds not found in nature, but which are synthetically accessible and have been shown to possess significant biological activity and proteolytic stability. Combinatorial libraries of cyclic compounds are disclosed wherein the cyclic compounds are comprised of at least one ring structure derived from cyclization of a peptoid backbone. The diversity of product compounds is generated by the sequential addition of substituted submonomers. The combinatorial library includes 10 or more, preferably 100 or more, and more preferably 1,000 or more distinct and different compounds. The library includes each of the product compounds in retrievable and analyzable amounts and preferably includes at least one biologically active compound. Methods of synthesizing the combinatorial libraries and assay devices produced using the libraries are disclosed as is methodology for screening for and obtaining biologically active cyclic organic compounds.