- Reduction of Electron-Deficient Alkenes Enabled by a Photoinduced Hydrogen Atom Transfer
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Direct hydrogen atom transfer from a photoredox-generated Hantzsch ester radical cation to electron-deficient alkenes has enabled the development of an efficient formal hydrogenation under mild, operationally simple conditions. The HAT-driven mechanism is supported by experimental and computational studies. The reaction is applied to a variety of cinnamate derivatives and related structures, irrespective of the presence of electron-donating or electron-withdrawing substituents in the aromatic ring and with good functional group compatibility. (Figure presented.).
- Larionova, Natalia A.,Ondozabal, Jun Miyatake,Cambeiro, Xacobe C.
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supporting information
p. 558 - 564
(2020/12/07)
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- Preparation method of cinacalcet hydrochloride and intermediate thereof
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The invention discloses a preparation method of cinacalcet hydrochloride and an intermediate thereof. The invention provides a preparation method of an intermediate L-cinacalcet tartrate III of cinacalcet hydrochloride. The method comprises the following steps: step (1): in an organic solvent, in the presence of a chiral catalyst and a chiral ligand, an asymmetric hydrogenation reduction reactionis conducted on a cinacalcet intermediate II to obtain cinacalcet IV, wherein the chiral catalyst is bis (1, 5-cyclooctadiene)-rhodium trifluoromethanesulfonate, and the chiral ligand is (S)-3, 3'-bis(2, 4, 6-triisopropylphenyl)-1, 1'-di-2-naphthol cyclic phosphate; and (2) in an organic solvent, a neutralization reaction is conducted between cinacalcet IV and L-tartaric acid to obtain L-cinacalcet tartrate III. The preparation method disclosed by the invention has advantages of short route step, simple and safe operation and high total yield; and the prepared product has high purity, meets the requirements of bulk drugs, is low in production cost and is suitable for industrial production.
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Paragraph 0086-0088
(2020/06/09)
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- Metal-Free Enantioselective Oxidative Arylation of Alkenes: Hypervalent-Iodine-Promoted Oxidative C?C Bond Formation
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The enantioselective oxyarylation of (E)-6-aryl-1-silyloxylhex-3-ene was achieved using a lactate-based chiral hypervalent iodine(III) reagent in the presence of boron trifluoride diethyl etherate. The silyl ether promotes the oxidative cyclization, and enhances the enantioselectivity. In addition, the corresponding aminoarylation was achieved.
- Shimogaki, Mio,Fujita, Morifumi,Sugimura, Takashi
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supporting information
p. 15797 - 15801
(2016/12/16)
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- Photodriven Transfer Hydrogenation of Olefins
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An improved practical method for the photodriven diimide reduction of olefins was investigated. This catalyst-free procedure proceeds at ambient temperature, utilizes air as oxidant and a lower hydrazine loading, and produces inert nitrogen gas as the sole byproduct. Several functional groups were tolerated, and in some cases, the reaction was chemoselective. Challenging substrates such as cinnamate ester derivatives and trans-stilbene were reduced in excellent yields. The small amount of UVA rays emitted from a household compact fluorescent light bulb was proposed to enable the cis/trans isomerization of the diimide and to promote the loss of hydrogen from the diimide.
- Leow, Dasheng,Chen, Ying-Ho,Hung, Tzu-Hang,Su, Ying,Lin, Yi-Zhen
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supporting information
p. 7347 - 7352
(2016/02/18)
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- A novel asymmetric synthesis of cinacalcet hydrochloride
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A novel route to asymmetric synthesis of cinacalcet hydrochloride by the application of (R)-tert-butanesulfinamide and regioselective N-alkylation of the naphthyl ethyl sulfinamide intermediate is described.
- Arava, Veera R.,Gorentla, Laxminarasimhulu,Dubey, Pramod K.
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p. 1366 - 1373
(2012/10/29)
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- PROCESS FOR CINACALCET HYDROCHLORIDE
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3-[3-(Trifluoromethyl)phenyl]propionaldehyde is a key intermediate for the preparation of cinacalcet hydrochloride. The present invention provides a novel process for the preparation of 3-[3-(trifluoromethyl)phenyl]propionaldehyde. The present invention also provides an improved process for preparation of cinacalcet hydrochloride in high yields. The present invention further provides a process for purification of cinacalcet hydrochloride.
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Page/Page column 11-12
(2012/02/02)
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- METHOD FOR PRODUCING PHENYLALKANE-1-OLS
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The present invention relates to a process for preparing phenylalkan-1-ols in three stages, where an ester condensation in the presence of alkali metal or alkaline earth metal alcoholates is carried out in the first stage.
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Page/Page column 4
(2011/06/10)
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- An investigation into the one-pot Heck olefination-hydrogenation reaction
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Herein is described an operationally simple process concerning the observation that, following either inter-, or intramolecular Heck olefination, stirring of the so formed substituted alkenyl product under an atmosphere of hydrogen efficiently effects alkene hydrogenation. Overall this two-operation, one-pot "reductive Heck" sequence is notable since direct reductive Heck processes, using additives such as formate salts, are restricted to a limited range of substrates. In total 25 examples are reported (yields ranging from 0 to 95%), which were selected in order to probe the scope and limitations of this method. Finally, the utility of this sequence was demonstrated in a short synthesis of the calcimimetic agent, cinacalcet.
- Geoghegan, Kimberly,Kelleher, Susan,Evans, Paul
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experimental part
p. 2187 - 2194
(2011/05/14)
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- PROMOTER FOR BICARBONATE SECRETION IN GASTROINTESTINAL TRACT
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Disclosed is a substance which can prevent or treat a disease associated with the secretion of an acid. A calcium receptor activator is used as an active ingredient of a promoter for the bicarbonate secretion in a gastrointestinal tract. Examples of the calcium receptor activator include γ-Glu-X-Gly [wherein X represents an amino acid or an amino acid derivative], γ-Glu-Val-Y [wherein Y represents an amino acid or an amino acid derivative], γ-Glu-Ala, γ-Glu-Gly, γ-Glu-Cys, γ-Glu-Met, γ-Glu-Thr, γ-Glu-Val, γ-Glu-Orn, Asp-Gly, Cys-Gly, Cys-Met, Glu-Cys, Gly-Cys, Leu-Asp, γ-Glu-Met(O), γ-Glu-y-Glu-Val, γ-Glu-Val-NH2, γ-Glu-Val-ol, γ-Glu-Ser, γ-Glu-Tau, γ-Glu-Cys(S-Me)(O), γ-Glu-Leu, γ-Glu-Ile, γ-Glu-t-Leu and γ-Glu-Cys(S-Me).
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- IMMUNOSTIMULATING AGENT
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Disclosed is an immunostimulating agent which can stimulate immunity effectively. The immunostimulating agent comprises, as an active ingredient, a calcium receptor activator such as γ-Glu-X-Gly [wherein X represents an amino acid or a derivative thereof other than Cys], γ-Glu-Val-Y [wherein Y represents an amino acid or a derivative thereof], γ-Glu-Ala, γ-Glu-Gly, γ-Glu-Met, γ-Glu-Thr, γ-Glu-Val, γ-Glu-Orn, Asp-Gly, Cys-Gly, Cys-Met, Glu-Cys, Gly-Cys, Leu-Asp, γ-Glu-Met(O), γ-Glu-y-Glu-Val, γ-Glu-Val-NH2, γ-Glu-Val-ol, γ-Glu-Ser, γ-Glu-Tau, γ-Glu-Cys(S-Me)(O), γ-Glu-Leu, γ-Glu-Ile, γ-Glu-t-Leu, γ-Glu-Cys(S-Me), a cation having a valency of 2 or more, protamine, polylysine, spermine, spermidine, putrescine, cinacalcet, a cinacalcet analogue compound, and a salt of any one of the aforementioned components.
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- DATA PROCESSING DEVICE, PARTICULARLY A SET-TOP BOX FOR CONNECTION TO A RECEIVER, INPUT DEVICE FOR THE CONTROL OF A DATA PROCESSING DEVICE, AND METHOD FOR OPERATING A DATA PROCESSING DEVICE
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The invention relates to a data processing device, particularly a set-top box, and a method for operating the data processing device (16). The data processing device (16) is provided for the connection to a receiver (15) and a communication network. The data processing device (16) is configured to receive and process data sent from the communication network, comprising content data (2) and at least one identification date (3), and to transmit the processed data to the receiver (15) for the output thereof. The data processing device (16) is further configured to receive and process a code sent by an input device of the data processing device and/or of the receiver (15), the code being associated with a certain identification date (3) of the identification data. In response to the receipt of the code, a communication connection is established between the data processing device (16), or a communication terminal (19), and a unit of the communication network, which is associated with the certain identification date (3).
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Page/Page column 25
(2008/06/13)
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- Synthesis and in vitro evaluation of human FP-receptor selective prostaglandin analogues
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The in vitro evaluation of a series of saturated prostaglandins revealed that compounds with omega chin aromatic rings retain nanomolar potency for the human prostaglandin F receptor (hFP receptor), exemplified by compound 8. In contrast, the double bonds are required for activity in the series with an acyclic omega chain as in PGF(2α). (C) 2000 Published by Elsevier Science Ltd.
- DeLong, Mitchell A.,Amburgey, Jack,Taylor, Cynthia,Wos, John A.,Soper, David L.,Wang, Yili,Hicks, Renee
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p. 1519 - 1522
(2007/10/03)
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