503417-37-6Relevant articles and documents
Process development and pilot-plant synthesis of (S)-tert-butyl 1-oxo-1-(1-(pyridin-2-yl)cyclopropylamino)propan-2-ylcarbamate: Studies on the scale-up of Kulinkovich-Szymoniak cyclopropanation
Li, Wenjie,Gao, Joe J.,Lorenz, Jon C.,Xu, Jinghua,Johnson, Joe,Ma, Shengli,Lee, Heewon,Grinberg, Nelu,Busacca, Carl A.,Lu, Bruce,Senanayake, Chris H.
, p. 836 - 839 (2012)
A practical and scalable synthesis of (S)-tert-butyl 1-oxo-1-(1-(pyridin-2- yl)cyclopropylamino)propan-2-ylcarbamate, an intermediate in the manufacture of a lymphocyte function-associated antigen 1 inhibitor, is described. The titled compound is prepared via an efficient one-pot, two-step telescoped sequence starting from readily available materials. A modified Kulinkovich-Szymoniak cyclopropanation of a nitrile followed by in situ amide formation with an activated carboxylic acid derivative afforded the target product in about 50% overall isolated yield and >97% purity.
5-FLUORONICOTINAMIDE DERIVATIVES AND USES THEREOF
-
Paragraph 00454-00457, (2021/04/10)
Provided herein is a compound of Formula (I), or pharmaceutically acceptable salt thereof, wherein R1, Y, X, and n are defined herein. Also provided herein are compositions comprising a compound of Formula (I) or pharmaceutically acceptable salt thereof, and methods of using a compound of Formula (I) or pharmaceutically acceptable salt thereof, e.g., in the treatment of heart disease.
PIPERAZINE AND HOMOPIPERAZINE DERIVATIVES AS HIV ATTACHMENT INHIBITORS
-
Page/Page column 63, (2014/10/15)
Compounds of Formula I, including pharmaceutically acceptable salts thereof, are useful as HIV attachment inhibitors.
BICYCLIC PYRIDINES AND ANALOGS AS SIRTUIN MODULATORS
-
Page/Page column 77, (2011/06/16)
Provided herein are novel sirtuin-modulating compounds and methods of use thereof. The sirtuin-modulating compounds may be used for increasing the lifespan of a cell, and treating and/or preventing a wide variety of diseases and disorders including, for example, diseases or disorders related to aging or stress, diabetes, obesity, neurodegenerative diseases, cardiovascular disease, blood clotting disorders, inflammation, cancer, and/or flushing as well as diseases or disorders that would benefit from increased mitochondrial activity. Also provided are compositions comprising a sirtuin-modulating compound in combination with another therapeutic agent.
ARYL-AND HETARYLSULFONAMIDES AS ACTIVE INGREDIENTS AGAINST ABIOTIC PLANT STRESS
-
Page/Page column 36-37, (2011/10/10)
Use of substituted sulfonamides of the formula (I) or salts thereof for enhancing stress tolerance in plants to abiotic stress, especially for enhancing plant growth and/or for increasing plant yield.
ISOXAZOLINE-SUBSTITUTED BENZAMIDE COMPOUND AND PEST CONTROL AGENT
-
Page/Page column 92, (2010/03/02)
Novel pest control agents, particularly insecticides or miticides are provided. Isoxazoline-substituted benzamide compounds of General Formula (1) or a salt thereof: (where A1, A2 and A3 are independently C or N, G is a benzene ring, etc., Q is a structure of Q-1, Q-2 or Q3: (where, for example, R1 in Q-1 is a C1 to C4 haloalkyl, etc., and R2 is H, etc., R1 in Q-2 is -OR1a, etc., R1a is a C1 to C4 alkyl, etc., and R2 is H, etc.), W is O or S, X is a halogen atom, a C1 to C2 haloalkyl, etc., Y is a halogen atom, a C1 to C2 alkyl, etc., R3 is a C1 to C2 haloalkyl, etc., m is an integer of 1-3, etc., and n is an integer of 0 or 1, etc.,), and pest control agents containing the copmpounds.
COMPOUNDS FOR TREATING VIRAL INFECTIONS
-
, (2008/12/08)
The invention relates to compounds, pharmaceutical compositions and methods useful for treating viral infection.
PYRAZOLE DERIVATIVES
-
Page/Page column 65, (2010/11/26)
A compound represented by formula (I): (wherein Ar1 represents a phenyl group which may have 1 to 3 substituents, or a non-substituted 5- or 6-membered aromatic heterocyclic group; Ar2 represents (i) a non-substituted phenyl group, (ii) a phenyl group which has been substituted by a lower alkyl group having 1 to 3 groups or atoms selected from among a carbamoyl group, an amino group, a hydroxyl group, a lower alkoxy group, and a halogen atom, or (iii) a 5- or 6-membered nitrogen-containing aromatic heterocyclic group which has been substituted by 1 to 3 groups or atoms selected from among a lower alkyl group, a lower alkynyl group, a lower alkanoyl group, a carbamoyl group, a cyano group, an amino group, a hydroxyl group, a lower alkoxy group, and a halogen atom; and X represents a group represented by formula (II): (wherein the ring structure represents a 4- to 7-membered heterocyclic group which may have, in addition to the nitrogen atom shown in formula (II), one heteroatom selected from among nitrogen, oxygen, and sulfur, and which may be substituted by 1 to 4 groups or atoms selected from among a lower alkyl group, a carbamoyl group, an amino group, a hydroxyl group, a lower alkoxy group, an oxo group, a lower alkanoyl group, a lower alkylsulfonyl group, and a halogen atom)), a salt thereof, a solvate of the compound or the salt, and a drug.
Primary 1-Arylcyclopropylamines from aryl cyanides with diethylzinc and titanium alkoxides
Wiedemann, Stefan,Frank, Daniel,Winsel, Harald,De Meijere, Armin
, p. 753 - 755 (2007/10/03)
(Matrix presented) 1-Aryl-substituted primary cyclopropylamines are conveniently prepared from aromatic nitriles and diethylzinc. The yields range from 40 to 56% for donor-substituted (five examples) to 62-82% for non- and acceptor-substituted substrates
