专利号:WO-0140193-A1 优先权日:1999-12-03 标题:Method for the synthesis of pyrazolines 发明人:BOLDI ARMEN M 权利人:CHEMRX ADVANCED TECHNOLOGIES I; BOLDI ARMEN M 摘要:The present invention provides a method for the synthesis of compounds of Formula (I). Also claimed are novel intermediates and their methods of synthesis.
专利号:US-2002103381-A1 优先权日:2000-11-30 标 题 :Method for the synthesis of pyrazolines 发明人:BOLDI ARMEN M 摘要:The present invention provides a method for the synthesis of compounds of Formula I: n n n Also claimed are novel intermediates and their methods of synthesis.
专利号:US-3985835-A 优先权日:1973-07-30 标题 :Halogenated esters of phosphorus-containing acids 发明人:D ALELIO GAETANO F 权利人:ALELIO GAETANO F D 摘要:This invention deals with new phosphorus-containing esters having the formula R'''2NP(O) (ORCX=CXR')2 wherein X represents Cl or Br; R represents a divalent hydrocarbon radical of 1-20 carbon atoms; R' represents H, X or R''; R'' represents a monovalent hydrocarbon radical of 1-20 carbon atoms; R''' represents hydrogen, a monovalent hydrocarbon radical of 1-20 carbon atoms, a divalent saturated aliphatic hydrocarbon group having 5 carbon atoms between valencies and forming a cyclic structure with the N, or a derivative of said monovalent hydrocarbon radical in which the derivative group is hydroxy, NH2, NHR'', NR''2, -NR''''K, R''''NHNHC(O)-, R''''NHC(O)NH-, -(N-R-)n-NR'''' , ¦¦ KK R''COO-, R''CONH- or R''O, R'''' represents hydrogen or R''; n represents an integer having a value of 0-50; and K represents hydrogen, R'' or -P(O) (ORCX=CXR')2. These new esters are useful particularly as fire retardants, agricultural chemicals, fuel additives, plasticizers, monomers and intermediates for the synthesis of other useful derivatives.
专利号:US-2003092064-A1 优先权日:2001-04-05 标题 :System for the synthesis of spatially separated libraries of compounds and methods for the use thereof 发明人:READER JOHN C 权利人:MILLENNIUM PHARM INC 摘要:Featured is an apparatus useful for preparing combinatorial libraries of compounds in a parallel fashion so that the individual compounds of the library are spatially separate and the position of each compound of the library in the apparatus is known. Moreover, the apparatus is useful for the preparation of combinatorial libraries of compounds where the library is constructed from three or more building blocks, e.g., three, four, five, six or seven building blocks, resulting in a three, four, five, six or seven dimensional combinatorial library. Also featured are related methods for the preparation of three, four, five, six or seven dimensional combinatorial libraries of compounds using the apparatus of the present invention.
专利号:US-9422321-B2 优先权日:2010-09-07 标题 :Pyrimidine nucleoside derivatives, synthesis methods and uses thereof for preparing anti-tumor and anti-virus medicaments 发明人:CHANG JUNBIAO; AN HAOYUN; YU XUEJUN; GUO XIAOHE 权利人:CHANG JUNBIAO; AN HAOYUN; YU XUEJUN; GUO XIAOHE; HIGH & NEW TECH RES CENTER HENAN ACAD OF SCIENCES; ZHENGZHOU GRANLEN PHARMATECH LTD; UNIV ZHENGZHOU 摘要:The present invention relates to the field of pharmacochemistry. Disclosed are fluorinated and azido-substituted pyrimidine nucleoside derivatives, particularly compounds of the formula shown below: n nAlso disclosed are methods of preparation and uses for these compounds. The compounds can be used for preparing medicaments for treating diseases such as tumors and viral infections, and can be used separately or in combination with other medicaments. The compounds also have effective activity against diseases such as tumors and viral infections, while having few side effects, and thus have potential application value.
专利号:US-6096874-A 优先权日:1990-10-01 标 题:High affinity tamoxifen derivatives 发明人:WALLACE SIDNEY; YANG DAVID; DELPASSAND EBRAHIM; CHERIF ABDALLAH; QUADRI SYED M 权利人:UNIV TEXAS 摘要:The synthesis of tamoxifen derivatives, most particularly halo, halo alkyl, hydroxy, and amino tamoxifen derivatives is disclosed. The native tamoxifen molecule includes a substituted chemical group positioned on the aliphatic chain of the tamoxifen molecule. Particular tamoxifen derivatives of the invention include chloro, bromo, iodo, fluoro, amino and DTPA tamoxifen derivatives, and corresponding lower alkyl halogenated forms. The halogenated tamoxifen derivatives possess superior binding affinities for estrogen receptor rich tissues, such as uterine tissue and breast tissue, relative to unsubstituted native tamoxifen. Radiolabeled forms of the tamoxifen derivatives may be used as highly specific imaging agents for estrogen receptor rich tissues. The fluoro and bromo tamoxifen derivatives are particularly useful for imaging estrogen receptors by PET whereas the iodinated tamoxifens are particularly useful in imaging estrogen receptors by SPECT. Rapid and efficient methods of preparing the tamoxifen derivatives having high specific activity (>6 Ci/μmol) are also disclosed. Aliphatic chain substituted tamoxifen derivatives are shown to possess greater estrogen receptor binding affinity and more potent tumor cell inhibition than tamoxifen or tamoxifen derivatives substituted at other locations on the molecule (i.e., non-aliphatic chain substituted tamoxifen). The tanioxifen derivatives of the present invention may advantageously be used as anti-cancer therapeutic agents to halt estrogen-receptor positive tumors, such as those of breast and uterine tissue. The present invention also provides a hydrophilic DTPA-tamnoxifen analogue, and uses thereof in imaging estrogen receptor positive ER+ lesions.
[参考文献]: Cristina Gabellieri, Et Al. Dynamic Nuclear Polarization With Polychlorotriphenylmethyl Radicals: Supramolecular Polarization-Transfer Effects. Angew Chem Int Ed Engl. 2010 Apr 26;49(19):3360-2.
合成参考文献
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