- Visible-Light-Driven Synthesis of Arylstannanes from Arylazo Sulfones
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The visible-light-driven preparation of (hetero)aryl stannanes was carried out under both photocatalyst- and metal-free conditions via irradiation of arylazo sulfones in the presence of hexaalkyldistannanes. The reaction shows a high efficiency and a wide substrates scope. The resulting crude organotin derivatives can be directly employed in a Stille protocol.
- Lian, Chang,Yue, Guanglu,Mao, Jinshan,Liu, Danyang,Ding, Yi,Liu, Zerong,Qiu, Di,Zhao, Xia,Lu, Kui,Fagnoni, Maurizio,Protti, Stefano
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supporting information
p. 5187 - 5191
(2019/07/03)
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- 1,2-AZABORINE COMPOUNDS AND SYNTHESIS
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A compound, or a pharmaceutically acceptable salt or ester thereof, having a structure of formula (I), wherein R1 is a substituted aryl or an optionally-substituted heteroaryl, provided that the heteroaryl is not pyridyl or azaborine; and each
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Page/Page column 15-16
(2014/02/16)
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- NOVEL METHOD OF PREPARING BENZOIMIDAZOLE DERIVATIVES
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This invention relates to a method of preparing a benzoimidazole derivative at high purity and high yield so as to enable the production of the benzoimidazole derivative compound as an antagonist against a vanilloid reactor-1, and particularly to a method
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Paragraph 0064
(2013/09/12)
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- Rhodium-catalyzed boron arylation of 1,2-azaborines
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A Sn-phony in B! BN isosteres of biphenyl compounds are prepared through Rh-catalyzed cross-coupling between 2-chloro-1,2-azaborines and arylstannanes (see scheme). The synthetic method should enable investigations of structure-activity relationships (SAR
- Rudebusch, Gabriel E.,Zakharov, Lev N.,Liu, Shih-Yuan
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supporting information
p. 9316 - 9319
(2013/09/12)
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- Synthesis of aryl trimethylstannanes from aryl amines: A sandmeyer-type stannylation reaction
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Sandmeyer-type stannylation: Stille coupling is one of the most powerful coupling reactions for C-C bond formation, whereas there are only limited methods to access aryl stannane compounds. A mild stannylation process based on a Sandmeyer-type transformation using aromatic amines as the starting materials is described. DCE: 1,2-dichloroethane. Copyright
- Qiu, Di,Meng, He,Jin, Liang,Wang, Shuai,Tang, Shengbo,Wang, Xi,Mo, Fanyang,Zhang, Yan,Wang, Jianbo
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supporting information
p. 11581 - 11584
(2013/11/06)
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- NOVEL METHOD OF PREPARING BENZOIMIDAZOLE DERIVATIVES
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This invention relates to a method of preparing a benzoimidazole derivative at high purity and high yield so as to enable the production of the benzoimidazole derivative compound as an antagonist against a vanilloid reactor-1, and particularly to a method
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Page/Page column 9
(2012/04/17)
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- Palladium-catalyzed carbostannylation by means of reagents containing carbon-tin-halogen inter-element linkages
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Reagents containing carbon-tin-halogen inter-element linkages were effective for palladium-catalyzed carbostannylation. In situ generated allyltin trichlorides add to carbon-carbon double bonds of bicyclo[2.2.1]hept-2-ene (norbornene) and bicyclo[2.2.1]hepta-2,5-diene (norbornadiene), stereoselectively, under the catalysis of palladium(0) species in good yields. The regioselectivity of unsymmetrically substituted allylic reagents dramatically alters with the choice of the tin(II) salt. Aryltin trichlorides undergo palladium-catalyzed arylstannylation of norbornene, giving a mixture of products composed of that taking one norbornene and that taking two norbornenes. The product ratio is dependent on the choice of the solvent and electronic nature of the aromatic substituent.
- Fugami, Keigo,Kawata, Kentaro,Enokido, Tatsuki,Mishiba, Yukie,Hagiwara, Sachiko,Hirunuma, Yasuyuki,Koyama, Daisuke,Kameyama, Masayuki,Kosugi, Masanori
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p. 433 - 444
(2007/10/03)
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- Arylation of organotin halides with pentaarylantimony and pentaphenylbismuth
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Pentaarylantimony and pentaphenylbismuth arylate oranotin halides R3SnX and R2SnX2 (R = Alk, Ar; X = Cl, Br) in toluene at room temperature to aryltin derivatives R3SnAr and R2SnArX (initial reagent molar ratio 1:1) or R2SnAr2 (2:1) in 78-95% yield.
- Sharutin,Sharutina,Senchurin,Kovaleva,Shcherbakov,Gladyshev
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- Benzo-fused lactams promote release of growth hormone
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There are disclosed certain novel compounds identified as benzo-fused lactams which promote the release of growth hormone in humans and animals. This property can be utilized to promote the growth of food animals to render the production of edible meat products more efficient, and in humans, to increase the stature of those afflicted with a lack of a normal secretion of natural growth hormone. Growth promoting compositions containing such benzo-fused lactams as the active ingredient therefore are also disclosed.
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- Benzo-fused lactams promote release of growth hormone
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There are disclosed certain novel compounds identified as benzo-fused lactams which promote the release of growth hormone in humans and animals. This property can be utilized to promote the growth of food animals to render the production of edible meat products more efficient, and in humans, to increase the stature of those afflicted with a lack of a normal secretion of natural growth hormone. The compounds are prepared by substitution of an amino-lactam with a substituted amide function. Growth promoting compositions containing such bezno-fused lactams as the active ingredient thereof are also disclosed. STR1 where L is STR2
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- Benzo-fused lactams promote release of growth hormone
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There are disclosed certain novel compounds identified as benzo-fused lactams which promote the release of growth hormone in humans and animals. This property can be utilized to promote the growth of food animals to render the production of edible meat products more efficient, and in humans, to increase the stature of those afflicted with a lack of a normal secretion of natural growth hormone. Growth promoting compositions containing such benzo-fused lactams as the active ingredient thereof are also disclosed.
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- SUBSTITUTED CARBAMOYL AND OXYCARBONYL DERIVATIVES OF BIPHENYLMETHYLAMINES
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Carbamoyl and oxycarbonyl derivatives of biphenylmethylamines of structure I are angiotensin-II antagonists with balanced AT 1 and AT. sub.2 activity useful in the treatment of hypertension and related disorders and ocular hypertension. STR1 where X is--O
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- SUBSTITUTED 1,2,4-TRIAZOLES BEARING ACIDIC FUNCTIONAL GROUPS AS ANGIOTENSIN II ANTAGONISTS
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Novel substituted triazolinone, triazolinethione, and triazolinimine compounds of the formula I are useful as angiotensin II antagonists. STR1
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- SUBSTITUTED PYRIDOPYRIMIDINONES AND RELATED HETEROCYCLES AS ANGIOTENSIN II ANTAGONISTS
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Novel substituted pyridopyrimidinones of formula (I), which are useful as angiotensin II antagonists, are disclosed. STR1
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- Benzo-fused lactams promote release of growth hormone
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There are disclosed certain novel compounds identified as benzo-fused lactams which promote the release of growth hormone in humans and animals. This property can be utilized to promote the growth of food animals to render the production of edible meat products more efficient, and in humans, to increase the stature of those afflicted with a lack of a normal secretion of natural growth hormone. The compounds are prepared by substitution of an amino-lactam with a substituted amide function. Growth promoting compositions containing such benzo-fused lactams as the active ingredient thereof are also disclosed. STR1 Where L is STR2
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- IMIDAZOLE DERIVATIVES BEARING ACIDIC FUNCTIONAL GROUPS AT THE 5-POSITION, THEIR COMPOSITIONS AND METHODS OF USE AS ANGIOTENSIN II ANTAGONISTS
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There are disclosed substituted imidazole derivatives of Formula I bearing acidic functional groups which are useful as angiotensin II antagonists. STR1
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- SUBSTITUTED PYRAZOLES, COMPOSITIONS AND USE
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Substituted pyrazole compounds are angiotensin II antagonists and therefore useful in the treatment of hypertension, and related cardiovascular disorders and ocular hypertension. These compounds have the general formula I: STR1
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- 6-AMINO SUBSTITUTED IMIDAZO[4,5-BIPYRIDINES AS ANGIOTENSIN II ANTAGONISTS
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Substituted imidazo[4,5-b]pyridines of structural formula: STR1 are angiotensin II antagonists useful in the treatment of hypertension and congestive heart failure.
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- Substituted pyrimidinones bearing acidic functional groups as angiotensin II antagonists
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Novel substituted fused pyrimidinones of formula (I) are useful as angiotensin II antagonists. STR1
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- SUBSTITUTED QUINAZOLINONES BEARING ACIDIC FUNCTIONALGROUPS AS ANGIOTENSIN II ANTAGONISTS
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Novel substituted quinazolinones of the formula (I) are useful as angiotensin II antagonists. STR1
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- Benzo-fused lactams that promote the release of growth hormone
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There are disclosed certain novel compounds identified as benzo-fused lactams which promote the release of growth hormone in humans and animals. This property can be utilized to promote the growth of food animals to render the production of edible meat products more efficient, and in humans, to increase the stature of those afflicted with a lack of a normal secretion of natural growth hormone. Growth promoting compositions containing such benzo-fused lactams as the active ingredient thereof are also disclosed.
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- IMIDAZOLE ANGIOTENSIN II ANTAGONISTS INCORPORATING ACIDIC FUNCTIONAL GROUPS
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There are disclosed substituted imidazole derivatives of Formula I which are useful as angiotensin II antagonists. STR1
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- Substituted 1-(2H)-isoquinolinones bearing acidic functional groups as angiotensin II antagonists
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Substituted 1-(2H)-isoquinolinones of the structural formula: STR1 are angiotensin II antagonists which are useful in the treatment of hypertension and congestive heart failure.
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- Reactions of Trialkylstannane Anions R3Sn- with Arylstannanes ArSnR'3
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The reactions of trialkylstannane anions R3Sn- with arylstannanes ArSnR'3 have been investigated; trialkylstannane anions with arylstannanes at 50 deg C gave substitution products ArSnR3 in good yields.Most of these substitution products are diverted to r
- Mochida, Kunio
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p. 3299 - 3306
(2007/10/02)
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- SYNTHESIS AND SPECTROSCOPIC CHARACTERISTICS OF ARYLTRIMETHYL-SILICON, -GERMANIUM, AND -TIN COMPOUNDS
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The synthesis and spectroscopic characteristics of 28 para-substituted aryltrimethyl-silicon, -germanium, and -tin compounds are described.The infrared spectra show characteristic bands at 1245-1165 (methyl bend), 840-765 (methyl rock), and 1105-1020 (in-plane aromatic H bend) cm-1; the frequency of the last band was found to depend on the sum of the aromatic substituent masses, the presence or absence of metallic constituents in the substituent having little influence.The mass spectral fragmentation patterns are interpreted in terms of localization of positive charge on the metal atom, with subsequent bond cleavage behavior which obeys the rules for mass spectra of carbon compounds.
- Moerlein, S. M.
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- Reactions of organotin hydrides with lithium diisopropylamide and organolithiums. Reactivities of the intermediates and of the lithium hydride produced
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Equimolar lithium diisopropylamide (LDA) and trimethyltin hydride (TMTH) react in tetrahydrofuran (THF) to form diisopropylamine and (trimethylstannyl)lithium, but in diethyl ether or hexanes 2 mol of TMTH is required for complete reaction and the products are diisopropylamine, hexamethylditin, and lithium hydride. When organic halides are present in this reacting system, reduction to alkane or substitution to form the trimethylalkyltin may occur depending on the nature of the halide. These and other observations suggest that (trimethylstannyl)lithium is formed as an intermediate yielding the tetraalkyltin. Studies on the products and stoichiometries of the reductions of alkyl bromides in ether and hexanes suggest that three reducing agents may be involved: TMTH, [Me3Sn(H)N-i-Pr2]-, and [Me3SnSn(H)Me3]-. The latter predominates in ether, and either or both of the others predominate in hexanes. Formation of methylcyclopentane from 1-bromo-5-hexene suggests involvement of a free radical mechanism. When methyllithium is used instead of LDA in the reaction with TMTH, the products are tetramethyltin and lithium hydride. This reaction can also be diverted to reduction by the presence of primary bromides. Aryl bromides react in both systems, but the yields of either substitution or reduction products are low. The lithium hydride formed in these reactions is extremely reactive as a base as shown by a brief study of its reaction with weak carbon acids and amines and as a nucleophile by its reaction with hexamethylditin to form (trimethylstannyl)lithium in THF.
- Reimann, Werner,Kuivila, Henry G.,Farah, Dan,Apoussidis, Theodorus
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p. 557 - 565
(2008/10/08)
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- SYNTHESIS OF ORGANOTRIALKYLSTANNANES. THE REACTION BETWEEN ORGANIC HALIDES AND HEXAALKYLDISTANNANES IN THE PRESENCE OF PALLADIUM COMPLEXES
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The aryl halides YC6H4X (X=Br or I) have been shown to react with the distannanes (R3Sn)2 (R=n-Bu or Me) in toluene in the presence of or to give the compounds YC6H4SnR3 for (a) R=n-Bu, Y=H, p-OMe, o-Me, p-Me, m-Cl, p-Cl, m-CN, p-COCH3 and m-NO2, and (b) R=Me, Y=H, p-OMe, p-Me, p-CN, p-COCH3, m-NO2 and p-NO2.Benzyl halides YC6H4CH2X (X=Cl or Br) similarly give YC6H4CH2SnR3 for (a) R=n-Bu, Y=H, m-OMe, p-OMe, m-Cl, m-CN, and m-NO2, and (b) R=Me, Y=m-Cl, m-CN, p-CN and m-NO2.These reactions are of special value as preparative procedures in cases in which Grignard or organolithium reagents cannot be used.Allyl chloride and bromide were likewise shown to react with (n-Bu3Sn)2 to give CH2=CHCH2SnBu3, but n-BuCl and n-BuBr gave only a trace of n-Bu4Sn.The mixed dimetallo species n-Bu3SnSiMe3 was shown to react with aryl bromides YC6H4Br (X=H, p-OMe, p-Me, or p-Cl) to give the arylsilicon compounds YC6H4SiMe3, with no aryltin products.
- Azizian, Hormoz,Eaborn, Colin,Pidcock, Alan
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