CAS: 212755-83-4; 2-(Pyridin-2-yl)Malonaldehyde

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2-pyridineacetic acid N,N-dimethyl-formamide dimethyl acetalN,N-dimethyl-formamide dimethyl acetal 2-(pyridin-2-yl)propane-1,3-diol formic acid 2-(1-(2-fluoro-4-nitrophenyl)-1H-pyrazole-4-yl)pyridine

2-(2-吡啶)-1,3-丙二醇置于三氧化硫吡啶,三乙胺体系中,用 二氯甲烷,二甲基亚砜 用作溶剂,化学反应 1.5H,以34.2%的收率获得2-(2-吡啶基)丙二醛
参考文献:新型恶唑烷酮抗菌候选药物的探索性工艺开发和千克级合成
标题:新型恶唑烷酮抗菌候选药物的探索性工艺开发和千克级合成
摘要:为大规模制备新型恶唑烷酮抗菌候选药物1,开发了一种简洁,对环境无害且具有成本效益的途径.通过对区域异构体混合物21进行轻度脱氨,可以制备高纯度的关键中间体2-(1-(2-氟-4-硝基苯基)-1 H-吡唑-4-基)吡啶7.通过亲核snar反应,通过4-(吡啶-2-基)-1 H-吡唑-3-胺14与1,2-二氟-4-硝基苯的仲胺官能团的选择性c-n偶联制备混合物10在最佳条件下,伯胺基保持完整.通过改变进料方式,可以很好地控制脱氨步骤的气态氮释放速率和反应混合物温度,从而提供安全保障.优化的合成策略1的总收率为27.6%,包括仅通过五个固液分离进行的七个连续转化,显着改善了产物分离的后处理.该策略绕开了涉及任何中间产品以及最终api的耗时且费力的过程.这项研究提出了一种能够快速交付高纯度api的几千克api的方法.
Doi:10.1021/op500030V

专利信息

专利号:US-6891069-B1
优先权日:2004-01-30
标 题:Synthesis of 4-substituted phthalaldehyde
发明人：ZHU PETER C; WANG DER-HAW
权利人:ETHICON INC
摘要:Disclosed herein are methods of synthesizing a 4-substituted-benzene-1,2-carbaldehyde. In one aspect, a method may include reacting a 4-substituted-1,2-bis(dibromomethyl) benzene with sulfuric acid to form a reaction product, introducing a solid sodium bicarbonate into the reaction product, and hydrolyzing the reaction product to form a 4-substituted-benzene-1,2-carbaldehyde, after introducing the bicarbonate.

专利号:US-11225655-B2
优先权日:2010-04-16
标题:Bi-functional complexes and methods for making and using such complexes
发明人：GOULIAEV ALEX HAAHR; FRANCH THOMAS; GODSKESEN MICHAEL ANDERS; JENSEN KIM BIRKEBAEK
权利人:GOULIAEV ALEX HAAHR; FRANCH THOMAS; GODSKESEN MICHAEL ANDERS; JENSEN KIM BIRKEBAEK; NUEVOLUTION AS
摘要:The present invention is directed to a method for the synthesis of a bi-functional complex comprising a molecule part and an identifier oligonucleotide part identifying the molecule part. A part of the synthesis method according to the present invention is preferably conducted in one or more organic solvents when a nascent bi-functional complex comprising an optionally protected tag or oligonucleotide identifier is linked to a solid support, and another part of the synthesis method is preferably conducted under conditions suitable for enzymatic addition of an oligonucleotide tag to a nascent bi-functional complex in solution.

专利号:US-7476767-B2
优先权日:2004-01-30
标题:Alpha-hydroxy sulfonate aldehydes, germicidal compositions containing the alpha-hydroxy sulfonate aldehydes, or mixtures of alpha-hydroxy sulfonate aldehydes and phthalaldehydes, and methods of using the compounds or compositions for disinfection or sterilization
发明人：ZHU PETER C; ROBERTS CHARLES G; TRAN YVONNE
权利人:ETHICON INC
摘要:Disclosed herein are α-Hydroxy sulfonate aldehydes and synthesis methods therefor. Germicidal compositions including the α-hydroxy sulfonate aldehydes, are also disclosed. In one aspect, a germicidal composition may include a diluent, and a germicidally effective amount of a water-soluble germicidal compound including an aldehyde group and an α-hydroxy sulfonate group. The water-soluble compound may have a solubility of at least 5 (w/v) % in water. In a further aspect, the compound may include 1-hydroxy-3-oxo-2-phenyl-propane-1-sulfonic acid salt, (2-formyl-phenyl)-hydroxy-methane sulfonic acid salt, 1-hydroxy-2-(4-methanesulfonyl-2-nitro-phenyl)-3-oxo-propane-1-sulfonic acid salt, 2-bromo-1-hydroxy-3-oxo-propane-1-sulfonic acid salt, 2-chloro-1-hydroxy-3-oxo-propane-1-sulfonic acid salt, 2-(1-formyl-2-hydroxy-2-sulfo-ethyl)-isonicotinic acid salt, 2-benzooxazol-2-yl-1-hydroxy-3-oxo-propane-1-sulfonic acid salt, or 1-hydroxy-2-(4-methoxy-phenyl)-3-oxo-propane-1-sulfonic acid salt. Germicidal compositions including a mixture of an α-hydroxy sulfonate aldehyde and one or more phthalaldehydes, such as phthalaldehyde, isophthalaldehyde, terephthalaldehyde, or a combination thereof, are also disclosed. Methods of using the compounds or compositions for killing bacteria, disinfection, or sterilization, are also disclosed.

专利号:US-8624035-B2
优先权日:2008-10-22
标题 :Functionalized cyanine having a silane linker arm, a method of preparing thereof and uses thereof
发明人：CAPUTO GIUSEPPE; MILETTO IVANA; BERTOLINO CHIARA ALESSANDRA; MARTRA GIANMARIO; COLUCCIA SALVATORE
权利人:CAPUTO GIUSEPPE; MILETTO IVANA; BERTOLINO CHIARA ALESSANDRA; MARTRA GIANMARIO; COLUCCIA SALVATORE; UNIV DEGLI STUDI TORINO
摘要:A silane-modified cyanine of Formula (I) includes the valence tautomers thereof: wherein R 1 is a linear, saturated or unsaturated alkyl chain, having 1 to 30 carbon atoms, wherein one or more carbon atoms are optionally substituted by a 4-, 5- or 6-membered aromatic or non aromatic cyclic grouping of carbon atoms; R 8 and R 9 are independently selected from the group consisting of —OCH 3 , —OCH 2 CH 3 , —OCH 2 CH 2 CH 3 , —OCH(CH 3 ) 2 , —OCH 2 CH 2 OCH 3 , —Cl, —Br, —I, Formula (II), Formula (III), —N(CH 3 ) 2 , Formula (IV), Formula (V), methyl, ethyl, propyl, isopropyl. The synthesis method and the use as a fluorescent marker are for inorganic solid supports, for example silica nanoparticles, and/or for biomolecules such as peptides, antibodies, DNA, RNA, etc.

专利号:US-7892297-B2
优先权日:2003-08-12
标题 :Cyanin-type compounds having an alkynyl linker arm
发明人：CAPUTO GIUSEPPE
权利人:CYANINE TECHNOLOGIES S P A
摘要:Cyanine-type fluorescent dyes modified with an alkynyl linker arm of formula (I), suitable for the conjugation of biomolecules, such as for example nucleosides, nucleotides, oligonucleotides, nucleic acids, proteins, peptides, vitamins and hormones. A method and intermediates for the synthesis of the alkynyl cyanines of the invention are also described, as well as alkynyl cyanine-biomolecule conjugates and methods for preparing thereof. The alkynyl cyanines can be advantageously used as markers for biomolecules or as quenchers.

专利号:EP-1559704-A1
优先权日:2004-01-30
标 题 :Synthesis of 4-substituted phthalaldehyde