- MONOMER, POLYMER, RESIST COMPOSITION, AND PATTERNING PROCESS
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A polymer for resist use is obtainable from a monomer having formula (1) wherein R1 is H, CH3 or CF3, R2 and R3 are a monovalent hydrocarbon group, R4 to R9 are hydrogen or a monovalent hydrocarbon group, R10 is a monovalent hydrocarbon group or fluorinat
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Paragraph 0326-0329
(2017/10/31)
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- Pyrrolopyrimidine compounds containing substituted cyclopentyl group
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The invention relates to the field of pharmaceutical chemistry, provides pyrrolopyrimidine compounds containing a substituted cyclopentyl group, and concretely relates to compounds represented by formula A, and stereoisomers and pharmaceutically-acceptable salts thereof. The invention also relates to methods for preparing the pyrrolopyrimidine compounds containing a substituted cyclopentyl group, represented by formula A, a medicinal composition of the compounds, and a use of the compounds in treatment of Janus kinase mediated diseases.
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Paragraph 0129; 0130; 0131; 0132
(2018/01/11)
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- Developing a Biocascade Process: Concurrent Ketone Reduction-Nitrile Hydrolysis of 2-Oxocycloalkanecarbonitriles
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A stereoselective bioreduction of 2-oxocycloalkanecarbonitriles was concurrently coupled to a whole cell-catalyzed nitrile hydrolysis in one-pot. The first step, mediated by ketoreductases, involved a dynamic reductive kinetic resolution, which led to 2-hydroxycycloalkanenitriles in very high enantio- and diastereomeric ratios. Then, the simultaneous exposure to nitrile hydratase and amidase from whole cells of Rhodococcus rhodochrous provided the corresponding 2-hydroxycycloalkanecarboxylic acids with excellent overall yield and optical purity for the all-enzymatic cascade.
- Liardo, Elisa,Ríos-Lombardía, Nicolás,Morís, Francisco,González-Sabín, Javier,Rebolledo, Francisca
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p. 3366 - 3369
(2016/07/26)
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- E-Selective Horner-Wadsworth-Emmons reaction of 2-OBO-cyclopentanone for the synthesis of rac-N-Cbz-Gly-Ψ[(E)-CF=C]-Pro-OH dipeptide isostere
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The Horner-Wadsworth-Emmons reactions of ethyl 2-fluoro-2- diethylphosphonoacetate with 2-(4-methyl-2,6,7-trioxabicyclo[2.2.2]octan-1-yl) cyclopentanone (2-OBO-cyclopentanone) using n-butyllithium furnished the corresponding tetra-substituted fluoroolefin in an E-selective manner (E:Z = 95:5). A facile synthesis of rac-N-Cbz-Gly-Ψ[(E)-CF=C]-Pro-OH as a dipeptide isostere was achieved based on the E-selective Horner-Wadsworth-Emmons reaction.
- Sano, Shigeki,Matsumoto, Tomoya,Nakao, Michiyasu
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p. 4480 - 4483
(2014/08/05)
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- Non-Cp titanium alkoxide-based homolytic ring-opening of epoxides by an intramolecular hydrogen abstraction in β-titanoxy radical intermediates
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A low-valent titanium species derived in situ from Ti(O-i-Pr)4, Me3SiCl and Mg powder in tetrahydrofuran reacted with epoxides to selectively provide less hindered alcohols via a homolytic ring-opening of epoxides, in which the intermediate β-titanoxy radical intramolecularly abstracted a hydrogen atom from an alkoxy moiety in the titanium complexes.
- Kawaji, Tsuyoshi,Shohji, Noriaki,Miyashita, Kenji,Okamoto, Sentaro
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supporting information; experimental part
p. 7857 - 7859
(2011/09/15)
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- Enantioselective hydrogenation of β-keto esters catalyzed by P-chiral bis(dialkylphosphino)ethanes-Ru(II)
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Asymmetric hydrogenation of keto esters using a BisP*-RuBr2 catalyst is reported. High enantioselectivities up to 98% were achieved in the hydrogenation of β-keto esters.
- Yamano, Toru,Taya, Naohiro,Kawada, Mitsuru,Huang, Taisheng,Imamoto, Tsuneo
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p. 2577 - 2580
(2007/10/03)
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- Stereo- and chemoselective transfer hydrogenation of carbonyl groups with RuCl2(PPh3)3 and BINAP-Ru as catalysts and et3NH+H2PO2-·1,5H 2O as a hydrogen donor
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Using Et3NH+H2PO2-.1.5 H2O as a hydrogen donor, the RuCl2(Ph3P)3, RuCl2(PPh3)3 / C and BINAP-Ru proved highly active catalysts for transfer hydrogenation of ketones under milder conditions than other hydrogen donors. 2-Methyl-, 2-chloro-, 2-(ethoxycarbonyl)cyclohexanones and -cyclopentanones were reduced to the less stable axial alcohols in excellent diastereoisomeric excess (de: 90-100%), and the carbonyl group of α,β-unsaturated ketones was selectively reduced, in contrast with other hydrogen donors the C=C bond was reduced. Copyright
- Khai, Bui The,Arcelli, Antonio
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p. 6599 - 6602
(2007/10/03)
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- Enantioselective [2,3]-wittig rearrangement via a chiral boron ester enolate
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The first enantioselective [2,3]-Wittig rearrangement of α-(allyloxy)- acetates is described which involves a chiral boron enolate with a chiral bis-suifonamide ligand to afford the α-hydroxy-β-alkyl-γ,δ-unsaturated esters in a high enantioselectivity (>9
- Fujimoto, Katsuhiko,Matsuhashi, Chiho,Nakai, Takeshi
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p. 423 - 435
(2007/10/02)
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- Asymmetric hydrogenation of beta- or gamma-ketoesters and beta- or gamma-ketoamides
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β- or γ-Ketoesters and β- or γ-ketoamides are asymmetrically reduced with a Ru(II)-BINAP derived catalyst at about 40° C. and about 50N/mm2 of hydrogen in the presence of a strong acid.
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- PHOTOCYCLIZATION OF ENAMIDES. 38 REDUCTIVE PHOTOCYCLIZATION OF α-(METHYLTHIO)- AND α-(ARYLTHIO)ENAMIDES
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Reductive photocyclization of α-(methylthio)enamide (2) gave exclusively six-membered lactams (3) and (4) while the same reaction of α-(arylthio)enamides (6) and (12) was found to afford five-membered lactams (7) and (13) as major products.A novel total s
- Naito, Takeaki,Tanada, Hiromi,Suzuki, Yumiko,Saito, Haruko,Kiguchi, Toshiko,Ninomiya, Ichiya
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p. 2345 - 2366
(2007/10/02)
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- 65. Homogeneous and Heterogeneous Asymmetric Reactions. Part 5. Diastereoselective and Enantioselective Hydrogenation of Cyclic β-Keto Esters on Modified Raney-Nickel Catalysts
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The hydrogenations of methyl 2-oxocyclopentanecarboxylate (1), ethyl 2-oxocyclohexanecarboxylate (3), and 2-methylcyclohexanone (5) on unmodified Raney-Ni catalyst lead predominantly to the formation of the cis-hydroxy diastereoisomers of 2, 4, and 6, respectively (Scheme 2).In the asymmetric hydrogenations on catalysts modified with chiral tartaric acid (R,R)-C4H6O6/Raney-Ni and (R,R)-C4H6O6/NaBr/Raney-Ni), the predominance of the cis-isomer increases significantly.The hydrogenations of β-keto esters 1 and 3 proceed with an enantioselectivity of 10-15percent on the modified catalysts, while the similar hydrogenation of 5 yields optically inactive 6.The (1S,2R)-enantiomers of the cis-isomers of 2 and 4 are formed in larger quantity, whereas the (1R,2R)-enantiomers of the corresponding trans-isomers predominate (Scheme 1).The enantioselective formation of trans-2 and trans-4 can be interpreted mainly in terms of the asymmetric hydrogenation of cyclic β-keto esters through the keto form, while that of the corresponding cis-hydroxy esters proceeds through the enol form.
- Wittmann, Gyula,Goendoes, Gyoergy,Bartok, Mihaly
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p. 635 - 639
(2007/10/02)
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- Angiotensin Converting Enzyme Inhibitors as Antihypertensive Agents: 1--L-prolines
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The synthesis of 1--L-prolines, 1--L-prolines and related benzoyl derivatives as pure isomers is described.The abilities of all the compounds to inhibit angiotensin converting enzyme (ACE) in vitro and in vivo and to lower the systolic blood pressure in renal hypertensive dogs were determined.Three of them, namely 1-carbonyl>-L-proline (10f(R,S)), 1--L-proline (10g(R,S)), and 1-carbonyl>-L-proline (16f(R,S)), werefound to be as potent as captopril in reducing blood pressure.The influence of chirality and ring size on the ACE inhibition is described.
- Ciabatti, Romeo,Padova, Giovanna,Bellasio, Elvio,Tarzia, Giorgio,Depaoli, Adele,et al.
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p. 411 - 417
(2007/10/02)
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