CAS: 98-80-6; Phenylboronic Acid

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CAS号108-86-1 溴苯 | CAS号591-50-4 碘苯 | CAS号17763-67-6 三氟甲烷磺酰苯 | CAS号556-97-8 3,5-二甲基氯苯 | CAS号24388-23-6 苯硼酸频呐醇酯 | CAS号591-51-5 苯基锂 | CAS号73183-34-3 双戊酰二硼 | CAS号71-43-2 苯 | CAS号109674-45-5 苯硼酸MIDA酯 | CAS号22092-92-8 N,N-二异丙基氨基硼烷 | CAS号10477-94-8 3-甲基-5-苯基吡啶 | CAS号104636-54-6 5-Phenylindoline | CAS号103068-20-8 1-溴-3,5-二苯基苯 | CAS号1032373-56-0 methyl 4-amino-... | CAS号103012-26-6 3-苯基-9H-咔唑 | CAS号109496-98-2 5-苯基靛红 | CAS号108976-70-1 2',5'-DIMETHYL-... | CAS号106274-68-4 3-氨基联苯-2-甲腈 | CAS号100094-00-6 1-(bromomethyl)... | CAS号105902-32-7 4'-METHYL[1,1'-...

二苯基汞置于三氯化硼体系中,化学反应生成 苯硼酸
参考文献:Some Studies On The Preparation Of Arylboronic Acids1
标题:Some Studies On The Preparation Of Arylboronic Acids1
摘要:
DOI:10.1021/ja01547A032

专利信息

专利号:US-9388131-B2
优先权日:2011-04-27
标题:Automated synthesis of small molecules using chiral, non-racemic boronates
发明人：BURKE MARTIN D; LI JUNQI; GILLIS ERIC P
权利人:UNIV ILLINOIS
摘要:Provided are methods for making and using chiral, non-racemic protected organoboronic acids, including pinene-derived iminodiacetic acid (PIDA) boronates, to direct and enable stereoselective synthesis of organic molecules. Also provided are methods for purifying PIDA boronates from solution. Also provided are methods for deprotection of boronic acids from their PIDA ligands. The purification and deprotection methods may be used in conjunction with methods for coupling or otherwise reacting boronic acids. Iterative cycles of deprotection, coupling, and purification can be performed to synthesize chiral, non-racemic compounds. The methods are suitable for use in an automated chemical synthesis process. Also provided is an automated small molecule synthesizer apparatus for performing automated stereoselective synthesis of chiral, non-racemic small molecules using iterative cycles of deprotection, coupling, and purification.

专利号:US-9862733-B2
优先权日:2010-07-23
标题 :Apparatus and methods for the automated synthesis of small molecules
发明人：BURKE MARTIN D; GILLIS ERIC P; BALLMER STEVEN G
权利人:BURKE MARTIN D; GILLIS ERIC P; BALLMER STEVEN G; UNIV ILLINOIS
摘要:Provided are methods for purifying N-methyliminodiacetic acid (MIDA) boronates from solution. Also provided are methods for deprotection of boronic acids from their MIDA ligands. The purification and deprotection methods can be used in conjunction with methods for coupling or otherwise reacting boronic acids. Iterative cycles of deprotection, coupling, and purification can be performed to synthesize chemical compounds of interest. The methods are suitable for use in an automated chemical synthesis process. Also provided is an automated small molecule synthesizer apparatus for performing automated synthesis of small molecules using iterative cycles of deprotection, coupling, and purification in accordance with methods of the invention. Coupling and other reactions embraced by the invention include, without limitation, Suzuki-Miyaura coupling, oxidation, Swern oxidation, “Jones reagents†oxidation, reduction, Evans' aldol reaction, HWE olefination, Takai olefination, alcohol silylation, desilylation, p-methoxybenzylation, iodination, Negishi cross-coupling, Heck coupling, Miyaura borylation, Stille coupling, and Sonogashira copling.

专利号:WO-0027627-A1
优先权日:1998-11-12
标题 :Aryloxime linkers in the solid-phase synthesis of 3-aminobenzisoxazoles
发明人：WILEY MICHAEL ROBERT; LEPORE SALVATORE DONATO
权利人:LILLY CO ELI; WILEY MICHAEL ROBERT; LEPORE SALVATORE DONATO
摘要:In its first aspect, the invention is directed to a solid support mediated method for the synthesis of diverse polycyclic heterocycles according to general formula (V). A second aspect of the invention is directed to a solid support bound intermediate compound that optionally can be derivatized before a cyclization and displacement procedure provides a product. The intermediate is preferably stable to a wide range of chemical conditions thus allowing, if desired, for the chemical derivatization of the intermediate. A third aspect of the invention is directed to a library of polycyclic heterocycle compounds where said library contains a plurality of diverse library compounds of general formula (V). A fourth aspect of the invention is directed to a method for the synthesis of a library of diverse polycyclic heterocycles by the general method described. A fifth aspect of the invention is directed to an assay kit for the identification of lead compounds of the library described therein.

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.

专利号:US-2006287520-A1
优先权日:2005-05-16
标 题 :Synthesis of salinosporamide A and analogues thereof
发明人：DANISHEFSKY SAMUEL J; ENDO ATSUSHI
权利人:DANISHEFSKY SAMUEL J; ENDO ATSUSHI
摘要:A novel synthesis of salinosporamide A is provided. Salinospoamide A as well as structurally related natural products, omuralide and lactacystin, have been shown to be proteasome inhibitors. Therefore, these compounds as well as analogues of these natural products may be useful in the treatment of proliferative diseases such as cancer, autoimmune diseases, diabetic retinopathy, etc. The invention provides for the synthesis of salinosporamide A as well as analogs thereof using a convenient point for derivatization of the bicyclic core. Pharmaceutical compositions and method of using the inventive compounds are also provided.

专利号:US-2008103312-A1
优先权日:2006-08-29
标 题:Processes for the synthesis of 5-phenyl-1-trityl-1H-tetrazole
发明人：KANSAL VINOD K; MISTRY DHIRENKUMAR N; VASOYA SANJAY L; LUNAGARIYA VIJAYKUMAR D
权利人:KANSAL VINOD K; MISTRY DHIRENKUMAR N; VASOYA SANJAY L; LUNAGARIYA VIJAYKUMAR D
摘要:Provided are processes for the synthesis of 5-phenyl-1-trityl-1H-tetrazole, an intermediate useful in the synthesis of irbesartan.