Abstract:
Disclosed herein are a process and composition to make polymerizable resins containing oxazolidone, in which organic acid-catalyzed and/or thermal annealing process got involved and consequently promoted a unique intramolecular transformation from a linear urethane linkage to a cyclic urethane linkage for those specifically constructed urethane resins containing α-substituted β-ketone moieties. Disclosed herein are a process and composition to make polymerizable resins containing oxazolidone, in which organic acid-catalyzed and/or thermal annealing process got involved and consequently promoted a unique intramolecular transformation from a linear urethane linkage to a cyclic urethane linkage for those specifically constructed urethane resins containing α-substituted β- ketone moieties.
Abstract:
Phenyliodonium ylide derivatives substituted with electron donating as well as electron withdrawing groups on the aromatic ring are shown for use as precursors in aromatic nucleophilic substitution reactions. The iodonium ylide group is substituted by nucleophiles such as halide ions to provide the corresponding haloaryl derivatives. No- carrier-added [F-18]fluoride ion exclusively substitutes the iodonium ylide moiety in these derivatives and provides high specific activity F- 18 labeled fluoro derivatives. Protected L-dopa-6-iodonium ylide derivative have been synthesized as a precursors for the preparation of no-carrier-added 6-[F- 18]fluoro-L-dopa. The iodonium ylide group in this L-dopa.derivative is nucleophilically substituted by no-carrier-added [F-18]fluoride ion to provide a [F-18]fluoro intermediates which upon acid hydrolysis yielded 6-[F- 18]fluoro-L-dopa.
Abstract:
A novel process, novel process steps and novel intermediates useful in the synthesis of pharmaceutically active N-acylbiphenyl alanine compounds, in particular neutral endopeptidase (NEP) inhibitors.
Abstract:
Radiolabeled fluorinated compounds useful for imaging in the diagnosis of Parkinson's Disease are disclosed. Methods and kits for their synthesis are also disclosed.
Abstract:
In one aspect, the invention relates to compounds having the formula: (I) where R 1 -R 6 , a, b, Z, and X are as defined in the specification, or a pharmaceutically acceptable salt thereof. These compounds have neprilysin inhibition activity. In another aspect, the invention relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and processes and intermediates for preparing such compounds.
Abstract:
The present invention relates, generally, to asymmetric α-functionalization and to asymmetric α,α-bisfunctionalization of ketones and aldehydes and, in particular, to chiral auxiliaries suitable for use in effecting such functionalizations and to methods of using same.
Abstract:
The present invention relates to a process for the production of a hydroxyoxazolidinone of formula (I) wherein A represents optionally substituted phenyl; which process comprises the step of treating a hydroxythiazolidinone of formula (II) in which A is as defined for formula (I); with an oxidising agent. The compounds of formula (I) may be used as intermediates in the synthesis of herbicidally active compounds.
Abstract:
A compound of formula (I), where E is oxygen or sulphur; A is CR or N where R is hydrogen or hydrocarbyl; D completes a 5 or 6-membered non-aromatic heterocyclic ring which optionally contains additional heteroatoms selected from oxygen nitrogen or sulphur and which is optionally substituted by an optionally substituted lower hydrocarbyl group, or an optionally substituted heteroaryl group; R and R are each independently hydrogen, optionally substituted lower hydrocarbyl, or optionally substituted heteroaryl, or R and R together with the nitrogen atom to which they are attached, form a heterocyclic ring; Z represents halogen, optionally substituted lower hydrocarbyl, optionally substituted lower hydrocarbyloxy, optionally substituted lower hydrocarbylthio, hydrocarbylsulphinyl, or hydrocarbylsulphonyl, cyano, nitro, CHO, NHOH, ONR7'R7'', SF5, CO (optionally substituted lower hydrocarbyl), acylamino, COOR , SO2NR R , CONR R , OR or NR R where R , R , R , R , R , R and R are independently H or lower hydrocarbyl; R is hydrogen, SO2 lower hydrocarbyl or COR ; R and R are independently lower hydrocarbyl, lower hydrocarbyloxy or a group R ; R is OR , NR R , hydrogen or lower hydrocarbyl; R is lower hydrocarbyl, R and R are independently hydrogen or lower hydrocarbyl provided that when there are two or more substituents Z, they may be the same or different; and m is 0 or an integer from 1 to 5.
Abstract translation:式(I)化合物,其中E为氧或硫; A是CR 3或N,其中R 3是氢或烃基; D完成5或6元非芳族杂环,其任选地含有选自氧氮或硫的另外的杂原子,其任选被任选取代的低级烃基或任选取代的杂芳基取代; R 1和R 2各自独立地为氢,任选取代的低级烃基或任选取代的杂芳基,或R 1和R 2与它们所连接的氮原子一起形成杂环; Z表示卤素,任选取代的低级烃基,任选取代的低级烃氧基,任选取代的低级烃基硫代,烃基亚磺酰基或烃基磺酰基,氰基,硝基,CHO,NHOH,ONR7'R7“,SF5,CO(任选取代的低级烃基) COOR 7,SO 2 NR 8 R 9,CONR 10 R 11,OR 12或NR 13 R 14,其中R 7,R 7',R“ R“,R 9,R 10和R 11独立地为H或低级烃基; R 12是氢,SO 2低级烃基或COR 15; R 13和R 14独立地为低级烃基,低级烃氧基或R 12基团; R 15是OR 16,NR 17 R 18,氢或低级烃基; R 16是低级烃基,R 17和R 18独立地是氢或低级烃基,条件是当有两个或更多个取代基Z时,它们可以相同或不同; m为0或1〜5的整数。