Abstract:
A method and system for selectively fluorinating organic molecules on a target site wherein the target site is activated and then fluorinated are shown together with a method and system for identifying a molecule having a biological activity.
Abstract translation:用于选择性氟化靶位点上的有机分子的方法和系统,其中靶位点被激活然后氟化,连同用于鉴定具有生物活性的分子的方法和系统一起显示。 p >
Abstract:
The present invention provides three basic routes for the total synthesis of taxol having structure (I). The present invention also provides the intermediates produced in the above processes, processes for synthesizing these intermediates as well as analogues of taxol and nortaxol.
Abstract:
New process for the preparation of compounds of formula (I) in which R1 represents alkyl C1-5, in particular methyl, ethyl, propyl isopropyl, and the two radicals R2 represent independently of one another hydrogen or alkyl C1-5, in particular hydrogen or methyl, ethyl, propyl or isopropyl. The process is characterized by the hydrolysis of a compound of formula (II) in which R is alkoxy C1-4, chlorine, bromine or alcanoyloxy C1-4, R1 and R2 have the above meaning and R3 is alkyl C1-4, and by the fact that the compound obtained is subjected to aldol condensation and, in the case where R = alkoxy C1-4, the reaction compound is again subjected to acid treatment. The compounds of formula (I) are mainly aromatics.
Abstract:
The present disclosure provides compounds of the formula (I), (II), (III), wherein the variables are as defined herein for use in the treatment of fungal infections. In some embodiments, the fungal infection is an infection of Cryptococcus neojormans fungus. Also provided herein are compositions comprising a compound of formula I, II, or III and a second anti-fungal agent.
Abstract:
The discovery of distinct modes of asymmetric catalysis has the potential to rapidly advance chemists' ability to build enantioenriched molecules. As an example, the use of chiral cation salts as phase-transfer catalysts for anionic reagents has enabled a vast set of enantioselective transformations. A largely overlooked analogous mechanism wherein a chiral anionic catalyst brings a cationic species into solution is itself a powerful method. The concept is broadly applicable to a number of different reaction pathways, including to the enantioselective fluorocyclization of olefins, and dearomatization of aromatic systems with a cationic electrophile-transferring (e.g., fluorinating) agent and a chiral phosphate catalyst. The reactions proceed in high yield and stereoselectivity. The compounds and methods of the invention are of particular value, especially considering the scarcity of alternative approaches.
Abstract:
The present invention relates to compositions, for example, the DBU/Hexafluoroacetone hydrate salt, and processes of preparing and using the same for the modification of chemical compounds via the release of trifluoroacetate. The DBU/Hexafluoroacetone hydrate salt can perform trifluoromethylation reactions on chemical compounds, such as carbonyl group-containing compounds.
Abstract:
The present invention relates to a process for the preparation of compounds of formula (I), wherein the substituents are as defined in claim 1, by reacting a compound of formula (II), either with a chlorination or bromination agent or with a compound of formula (III) CI-SO 2 R 9 , R 9 being C 1 -C 4 alkyl, C 1 -C 4 haloalkyl, phenyl or C 1 -C 4 alkyl-substituted phenyl, to form the compound of formula (IV), reacting the compound of formula (IV) with a compound of formula (V) M + -O - -C(O)-Y, wherein Y is as defined above and M + is the hydrogen cation or an alkali metal ion, alkaline earth metal ion or ammonium ion, to form the compound of formula (VI) and treating that compound with a cyanide source in the presence of a base.
Abstract translation:本发明涉及一种制备式(I)化合物的方法,其中取代基如权利要求1所定义,通过使式(II)化合物与氯化或溴化剂或与 式(III)的化合物与式(Ⅳ)的化合物反应形成式(Ⅳ)的化合物,式(Ⅳ)的化合物与式 (V)M + O - C(O)-Y,其中Y如上定义,M +是氢阳离子或碱金属离子,碱土金属离子或铵离子,至 形成式(VI)的化合物,并在碱的存在下用氰化物源处理该化合物。
Abstract:
A highly pure 2,4,4,6-tetrabromo-2,5-cyclohexadienone has been prepared in a single pot, eco-friendly procedure in yields of 91-94 % from phenol. In this method, a mixture of alkali/alkaline earth metal bromide and alkali/alkaline earth metal bromate was employed as brominating agent in place of corrosive liquid bromine. The reaction between phenol and the brominating reagent was initiated by the action of a mineral acid or moderately strong organic acid. The crude product was further characterized by standard analytical and spectroscopic methods.