55162-34-0Relevant articles and documents
Synthesis of N-Alkyl Anilines from Arenes via Iron-Promoted Aromatic C-H Amination
Falk, Eric,Gasser, Valentina C. M.,Morandi, Bill
supporting information, p. 1422 - 1426 (2021/03/08)
We report both an intermolecular C-H amination of arenes to access N-methylanilines and an intramolecular variant for the synthesis of tetrahydroquinolines. A newly developed, highly electrophilic aminating reagent was key for the direct synthesis of unprotected N-methylanilines from simple arenes. The reactions display a broad functional group tolerance and employ catalytic amounts of a benign iron salt under mild reaction conditions.
BET INHIBITORS FOR MODULATING DUX4 EXPRESSION IN FSHD
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Page/Page column 84, (2020/07/14)
The present disclosure provides BET inhibitors of the formula: wherein the variables are defined herein, as well as pharmaceutical compositions thereof. The present disclosure also provides methods of treating a patient comprising administering a bromo- and extra-terminal (BET) domain inhibitor for the treatment of FSHD which modulates DUX4 expression. In some embodiments, the present methods comprise using one or more BET inhibitors as a therapeutic agent for the treatment of FSHD patients including patients who are being treated with one or more palliative treatments such as therapy and/or agents which lead to increased muscle mass.
Practical synthesis of a renin inhibitor via a diastereoselective dieckmann cyclization
Gauvreau, Danny,Hughes, Greg J.,Lau, Stephen Y. W.,McKay, Daniel J.,O'Shea, Paul D.,Sidler, Rick R.,Yu, Bing,Davies, Ian W.
supporting information; experimental part, p. 5146 - 5149 (2011/02/23)
A scalable synthesis of a potent renin inhibitor (1) is described. The absolute stereochemistry is set via an unprecedented diastereoselective Dieckmann cyclization directed by a remote chiral protecting group. This transformation enables preparation of chiral 1,3-[3.3.1]-diazabicyclononenes by desymmetrization of alkyl-esters, with selectivities ranging from 4 to 17:1.
ANTIBACTERIAL AGENTS
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Page/Page column 258, (2009/01/24)
Antibacterial compounds of formula (I) are provided, as well as stereoisomers, pharmaceutically acceptable salts, esters, and prodrugs thereof; pharmaceutical compositions comprising such compounds; methods of treating bacterial infections by the administration of such compounds; and processes for the preparation of such compounds.
A PROCESS FOR PREPARING DIAZABICYCLO[3.3.1] NONANE COMPOUNDS
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Page/Page column 17; 52, (2008/12/07)
The invention is a process for preparing a diazabicyclo compound of formula (I) process for preparing a diazabicyclo compound of formula (I):where X is selected from the group consisting of hydrogen, C1-C6 alkoxycarbonyl, and carbobenzyloxy; R6 is selected from the group consisting of C1-C6 alkyl, C2-C6 alkenyl, and benzyl; and R9, R 10, and R11 are independently selected from the group consisting of hydrogen, halogen, and C1-C6 alkyl. wherein the process involves cyclizing I-I, formula (II).
NOVEL CASE OF RENIN INHIBITORS
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Page/Page column 30-31, (2009/01/20)
The present invention relates to piperidine-based renin inhibitor compounds having carboxylate or carboxylic acid terminal groups. The disclosed low molecular weight, orally active renin inhibitors are of non-peptide nature and have long duration of action. The compounds can be used in the treatment of cardiovascular events and renal insufficiency.
SUBSTITUTED ACRYLAMIDE DERIVATIVE AND PHARMACEUTICAL COMPOSITION COMPRISING THE SAME
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Page/Page column 55, (2008/06/13)
A pharmaceutical composition comprising a compound having Formula (I) or a pharmacologically acceptable salt thereof as an active ingredient: [wherein, R1 is, for example, a C6-C10 aryl group which may be substituted with one group or more than one group selected from substituent group α; R2 is, for example, a C6-C10 aryl group which may be substituted with one group or more than one group selected from substituent group α; and X is, for example, a hydroxyl group or a C1-C6 alkoxy group].
SUBSTITUTED PROPANAMIDE DERIVATIVE AND PHARMACEUTICAL COMPOSITION CONTAINING THE SAME
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Page/Page column 65, (2008/06/13)
It is an object of the present invention to provide a substituted propanamide derivative or a pharmacologically acceptable salt thereof that is useful as a prophylactic or therapeutic agent for a bone metabolic disease. The present invention relates to a pharmaceutical composition comprising a compound having General Formula (I) or a pharmacologically acceptable salt thereof as an active ingredient: [wherein, R1 represents a C6-C10 aryl group that may be substituted by a group selected from Substituent Group α, for example; R2 represents a C6-C10aryl group that may be substituted by a group selected from Substituent Group α, for example; and X represents a hydroxyl group or a C1-C6 alkoxy group, for example].
Development of an efficient and stereoselective manufacturing route to idoxifene
Ace, Karl W.,Armitage, Mark A.,Bellingham, Richard K.,Blackler, Paul D.,Ennis, David S.,Hussain, Nigel,Lathbury, David C.,Morgan, David O.,O'Connor, Noah,Oakes, Graham H.,Passey, Stephen C.,Powling, Laurence C.
, p. 479 - 490 (2013/09/07)
A literature route to 1-(2-{4-[(E)-1-(4-iodophenyl)-2-phenyl-but-1-enyl]phenoxy}ethyl)pyrrolidine (idoxifene) has been modified to tackle various scale-up issues and provide initial supplies. A new highly efficient, robust, and stereoselective manufacturing route is described in detail. This route involves diastereoselective synthesis of tertiary alcohol (1RS,2SR)-1-(4-iodophenyl)-2-phenyl-1-[4-(2-pyrrolidin-1-yl-ethoxy)phenyl]butan- 1-ol by Grignard addition to the ketone 1-(4-iodophenyl)-2-phenyl-1-butanone followed by derivatisation and stereoselective syn elimination to provide idoxifene in excellent yield and geometric purity. Evaluation of a more direct route to idoxifene using a McMurry low-valent titanium coupling reaction is also described.
