cas 73096-42-1, 5-(2-BROMOPHENYL)-1H-TETRAZOLE

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Synthesis and characterization of magnetic Fe3O4@Creatinine@Zr nanoparticles as novel catalyst for the synthesis of 5-substituted 1H-tetrazoles in water and the selective oxidation of sulfides with classical and ultrasonic methods
Tetrazoles and sulfoxide compounds have a wide range of applications in industries and are of great expectation to be environmentally friendly and cost-effective. This paper reports the introduction of zirconium supported on Fe3O4 na
Ghadermazi, Mohammad,Moeini, Nazanin,Molaei, Somayeh
(2021/12/03)

Copper-based catalysts derived from salen-type ligands: Synthesis of 5-substituted-1: H-tetrazoles via [3+2] cycloaddition and propargylamines via A3-coupling reactions
Base-metal copper(ii) complexes derived from unsymmetrical salen-type ligands were designed and synthesized using ligands L1H to L4H in moderate yield. The synthesized unsymmetrical ligands L1H to L4H and the corresponding copper complexes (1-4) were characterized by UV-visible, IR and ESI-MS spectroscopic studies. Molecular structures of complexes 1, 2 and 4 were determined by X-ray crystallography. Copper complexes 1-4 were employed as catalysts for [3+2] cycloaddition and A3-coupling reactions. The mutual approach of salen-type ligands and metals via active participation of ligands allow to achieve the catalytic reactions. Reaction pathways were proposed and possible intermediate species during the catalytic cycle were successfully characterized by ESI-MS spectroscopic studies. This journal is
Singh, Anshu,Maji, Ankur,Mohanty, Aurobinda,Ghosh, Kaushik
p. 18399 - 18418
(2020/11/13)

TMSN3-Bu2Sn(OAc)2: A modified and mild reagent system for Wittenberger tetrazole-synthesis
Treatments of various nitriles with TMSN3 and Bu2Sn(OAc)2 at 30 °C in benzene for 60 h yielded the corresponding 5-substituted 1H-tetrazoles in good to excellent yields. This method is a mild and efficient alternative reagent system for Wittenberger tetrazole-synthesis that uses TMSN3 and Bu2SnO in toluene at high temperature (93–110 °C) for 24–72 h.
Yoneyama, Hiroki,Oka, Naoki,Usami, Yoshihide,Harusawa, Shinya
supporting information

(2020/01/21)

Cationic organotin cluster [t-Bu2Sn(OH)(H2O)]2 2+2OTf?-catalyzed one-pot three-component syntheses of 5-substituted 1H-tetrazoles and 2,4,6-triarylpyridines in water
The cationic organotin cluster [t-Bu2Sn(OH)(H2O)]2 2+2OTf? is easy to prepare and stable in air. The catalytic activity of [t-Bu2Sn(OH)(H2O)]2 2+2OTf? as a neutral organotin Lewis acid catalyst is probed through the one-pot three-component syntheses of 5-substituted 1H-tetrazoles from aldehydes, hydroxylamine hydrochloride and sodium azide, and of 2,4,6-triarylpyridines from aromatic aldehydes, substituted acetophenones and ammonium acetate. The reactions proceed well in the presence of 1?mol% of [t-Bu2Sn(OH)(H2O)]2 2+2OTf? in water and provide the corresponding 5-substituted 1H-tetrazoles and 2,4,6-triarylpyridines in good to excellent yields. The method reported has several advantages such as the catalyst being neutral, low catalyst loading and use of water as a green solvent.
Wang, Hongshe,Zhao, Weixing,Du, Juan,Wei, Fenyan,Chen, Qi,Wang, Xiaomei
(2019/08/20)

Humic acid as an efficient and reusable catalyst for one pot three-component green synthesis of 5-substituted 1: H -tetrazoles in water
Humic acid is a non toxic, inexpensive, easily available high-molecular weight polymer. A simple and facile one pot three-component synthesis of 5-substituted 1H-tetrazoles from aldehydes, hydroxyamine hydrochloride and sodium azide using humic acid as an efficient catalyst in water is described. The method reported has several advantages such as high to excellent yields, easy work-up, mild reaction conditions, use of water as a green solvent, and a commercially available, nontoxic and reusable catalyst.
Wang, Hongshe,Wang, Yichun,Han, Yinfeng,Zhao, Weixing,Wang, Xiaomei
p. 784 - 789
(2020/01/23)

Tin-Catalyzed Synthesis of 5-Substituted 1H-Tetrazoles from Nitriles: Homogeneous and Heterogeneous Procedures
The preparation of 5-substituted 1H-tetrazoles was efficiently achieved by reaction of trimethylsilylazide with nitriles using a triorganotin alkoxide precatalyst. The reaction mechanism was first investigated using a homogeneous tributyltin derivative and was explored through experimental investigations and DFT calculations. A heterogeneous version was then developed using a polymer-supported organotin alkoxide and afforded an efficient method for the preparation of tetrazoles in high yields with an easy work-up and a residual tin concentration in the desired products compatible for pharmaceutical applications (less than 10 ppm). (Figure presented.).
Chrétien, Jean-Mathieu,Kerric, Gaelle,Zammattio, Fran?oise,Galland, Nicolas,Paris, Michael,Quintard, Jean-Paul,Le Grognec, Erwan
supporting information
p. 747 - 757
(2019/01/04)

INHIBITORS OF MENAQUINONE BIOSYNTHESIS
Provided herein are compounds of Formula (I) and pharmaceuticals acceptable salts, solvates, hydrates, polymorphs, co-crystals, tautomers, stereoisomers, and prodrugs thereof. Also provided are pharmaceutical compositions, kits, and methods involving the inventive compounds for the treatment of an infectious disease (e.g., bacterial infection (e.g., tuberculosis, methicillin- resistant Staphylococcus aureus).
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Paragraph 00386

(2017/08/01)

[Cu(phen)(PPh3)2]NO3-catalyzed microwave-assisted green synthesis of 5-substituted 1H-tetrazoles
Abstract: An efficient synthetic methodology for construction of 5-substituted 1H-tetrazoles under microwave irradiation in green medium is described. With [Cu(phen)(PPh3)2]NO3 as catalyst and H2O-isopropyl alcohol (IPA) as reaction medium, various substituted nitriles underwent (3?+?2) cycloaddition reaction with NaN3 under microwave irradiation to provide corresponding 5-substituted 1H-tetrazoles in high yield. This method is not only efficient and general but also benefits from high functional group tolerance. This environmentally friendly synthetic methodology is visualized as an alternative to existing procedures, providing a simple route to privileged scaffolds.
Padmaja,Meena,Maiti, Barnali,Chanda, Kaushik
p. 7365 - 7374
(2017/09/06)

Triple reuptake inhibitors: Design, synthesis and structure–activity relationship of benzylpiperidine–tetrazoles
Monoamine transporters are important targets in the treatment of various central nervous disorders. Several limitations of traditional reuptake inhibitors, like delayed onset of action, insomnia, and sexual dysfunction, have compelled the search for safer, more effective compounds. In this study, we have sought to identify novel monoamine reuptake inhibitors. Based upon the docking study of compounds that we had reported previously, aromatic rings (A1) were modified to generate a novel series of benzylpiperidine–tetrazoles. Thirty-one compounds were synthesized and evaluated for their triple reuptake inhibition of serotonin, norepinephrine and dopamine. Triple reuptake inhibitor, compound 2q, in particular, showed potent serotonin reuptake inhibition, validating our design approach.
Paudel, Suresh,Min, Xiao,Acharya, Srijan,Khadka, Daulat Bikram,Yoon, Goo,Kim, Kyeong-Man,Cheon, Seung Hoon
p. 5278 - 5289
(2017/10/06)

Regioselective and stereoselective route to N2-β-tetrazolyl unnatural nucleosides via SN2 reaction at the anomeric center of Hoffer's chlorosugar
We are reporting a regioselective and stereoselective route to N2-β-tetrazolyl aromatic donor/acceptor unnatural nucleosides as new class of possible DNA base analogs. The SN2 substitution reaction at the anomeric center of Hoffer's chlorosugar with various 5-substituted aromatic tetrazoles in THF in presence of K2CO3 proceeds with regioselectivity at N2-tetrazoles and stereoselectivity at α-chlorosugar with very good yield. The stereoelectronic and steric effects play a crucial role for the observed outcome which is also supported from a theoretical (DFT) study. The methodology is simple, eco-compatible and the tetrazolyl unnatural nucleosides might find applications in decorating DNA for various biotechnological and DNA based material science applications.
Bag, Subhendu Sekhar,Talukdar, Sangita,Anjali
supporting information
p. 2044 - 2050
(2016/04/05)

Expeditious Synthesis of 2-Phenylquinazolin-4-amines via a Fe/Cu Relay-Catalyzed Domino Strategy
A highly efficient Fe/Cu relay-catalyzed domino protocol has been developed for the synthesis of 2-phenylquinazolin-4-amines from commercially available ortho-halogenated benzonitriles, aldehydes, and sodium azide. This elegant domino process involved con
Jia, Feng-Cheng,Zhou, Zhi-Wen,Xu, Cheng,Cai, Qun,Li, Deng-Kui,Wu, An-Xin
supporting information
p. 4236 - 4239
(2015/09/15)

An efficient synthesis of 5-substituted 1H-tetrazoles via B(C 6F5)3 catalyzed [3+2] cycloaddition of nitriles and sodium azide
A simple and efficient protocol is developed for the synthesis of 5-substituted 1H-tetrazole derivatives from various nitriles and sodium azide (NaN3) via [3+2] cycloaddition reaction using B(C6F 5)3 as a catalyst. The present synthetic method displayed significant advantages such as low catalyst loading, mild reaction conditions, low toxicity, easy work-up, high yields, and compatibility with other functional groups.
Prajapti, Santosh Kumar,Nagarsenkar, Atulya,Babu, Bathini Nagendra
p. 3507 - 3510
(2014/06/10)

Synthesis of 5-substituted 1H-tetrazoles catalyzed by ceric ammonium nitrate supported HY-zeolite
In this Letter we wish to report a simple and efficient synthetic protocol for the synthesis of 5-substituted 1H-tetrazole derivatives through the [2+3] cycloaddition of nitriles with sodium azide using ceric ammonium nitrate supported HY-zeolite as a novel catalyst. Excellent yields of the corresponding tetrazoles were obtained through this cost-effective protocol under aerobic conditions with shorter reaction time under mild reaction conditions.
Sivaguru, Paramasivam,Bhuvaneswari, Kaliyan,Ramkumar, Rangasamy,Lalitha, Appaswami
supporting information
p. 5683 - 5686
(2014/12/12)

Click chemistry for the synthesis of 5-substituted 1H-tetrazoles from boron-azides and nitriles
A novel and metal free catalysis of synthesizing 5-substituted 1H-tetrazoles through 1,3-dipolar cycloaddition of boron-azides and nitriles is reported with broad substrate scope and excellent yields.
Yao, Yue-Wei,Zhou, Yi,Lin, Bao-Ping,Yao, Cheng
supporting information
p. 6779 - 6781
(2013/11/19)

Green synthetic approach to 5-substituted-1h-tetrazoles via recycle and reuse of tributyltin chloride
A simple, safe and efficient process for the recycle of tributyltin chloride from tributyltin hydroxide is developed and its reuse in the synthesis of 5-substituted-1H-tetrazoles is successfully demonstrated, which paved a way to reduce the toxic tin waste significantly. Recycling of tributyltin chloride is possible over six cycles without loss of its activity.
Sampath,Reddy, V. Prabhakar,Chakravarthy, A. Kalyan,Reddy, P. Pratap
p. 393 - 396
(2013/02/22)

Phosphomolybdic acid (H3Mo12O40P) as a reusable heterogeneous catalyst for the synthesis of 5-substituted 1 H-Tetrazoles via [2+3] cycloaddition of nitriles and sodium azide
An efficient and practical protocol for the preparation of 5-substituted 1H-tetrazole derivatives is reported using phosphomolybdic acid as an effective heterogeneous catalyst. Good yields, simple methodology, and easy workup make this protocol more attractive for the diversity-oriented synthesis of these heterocycle libraries. The catalyst can be recycled three times with good yields.
Takale, Santosh,Manave, Smita,Phatangare, Kiran,Padalkar, Vikas,Darvatkar, Nitin,Chaskar, Atul
experimental part
p. 2375 - 2381
(2012/06/29)

Amine salt-catalyzed synthesis of 5-substituted 1H-tetrazoles from nitriles
The [3+2] cycloaddition reaction between sodium azide and various organic nitriles proceeds smoothly in the presence of amine salts as catalyst in dimethylformamide. The corresponding 5-substituted 1-H tetrazoles were obtained under mild condition in good to excellent yields. Supplemental materials are available for this article. Go to the publisher's online edition of Synthetic Communications to view the free supplemental file. Taylor & Francis Group, LLC.
Zhou, Yi,Yao, Cheng,Ni, Renjie,Yang, Gaowen
experimental part
p. 2624 - 2632
(2010/10/03)

Iron salts in the catalyzed synthesis of 5-substituted 1H-tetrazoles
A study was conducted to investigate the presence of iron salts in the catalyzed synthesis of 5-substituted 1H-tetrazoles. Para-trifluorotoluonitrile and trimethylsilyl azide were selected as model substrates for the initial metal source screening and the optimization of the reaction conditions. It was observed that the catalysis proceeded successfully producing tetrazole in 91% yield. A screening of various iron salts revealed that both the oxidation state of the iron and the counterion had a minor effect on the catalysis. Iron sources with different purity grades obtained from various providers were applied to investigate that the catalysis was not resulting from trace impurities in the metal salt. It was also observed that the catalysis proceeded successfully for a wide variety of aryl nitriles, providing tetrazoles in high yields. The best catalysis results were achieved with compounds that contained electron-withdrawing groups.
Bonnamour, Julien,Bolm, Carsten
supporting information; experimental part
p. 4543 - 4545
(2009/12/27)

1,3-Dipolar cycloaddition: Click chemistry for the synthesis of 5-substituted tetrazoles from organoaluminum azides and nitriles
Cheap and safe: Conventional methods to prepare tetrazoles employ dangerous, toxic reagents. A new route to these heterocycles (see scheme) uses inexpensive and nontoxic dialkyl aluminum azides. The cycloaddition occurs under mild conditions and tolerates a variety of functional groups. The low cost and ecocompatibility make this process attractive for large-scale preparation. (Chemical Equation Presented).
Aureggi, Valentina,Sedelmeier, Gottfried
p. 8440 - 8444
(2008/09/19)

Efficient synthesis of valsartan, a nonpeptide angiotensin II receptor antagonist
A highly efficient and convergent approach to the synthesis of the angiotensin II receptor antagonist valsartan (1), one of the most important agents used in antihypertensive therapy today, is described. Directed ortho-metalation of 4-bromotoluene provides the key boronic acid intermediate 11 which was subjected to palladium-catalyzed Suzuki coupling. This method overcomes many of the drawbacks associated with the previously reported syntheses. The saponification of the methyl ester in valsartan was realized in a convenient and economical manner, which is more suitable for industrial production. Georg Thieme Verlag Stuttgart.
Zhang, Chen,Zheng, Guojun,Fang, Lijing,Li, Yulin
p. 475 - 477
(2007/10/03)

THE USE OF SELECTIVE P2X7 RECEPTOR ANTAGONISTS
The present invention relates to the use of selective P2X7 receptor antagonists of formula (I), or a pharmaceutically acceptable salt or prodrug thereof wherein D, R1 and R2 are as defined in claim 1, for the treatment of neuropathic pain, chronic inflammatory pain, inflammation, neurodegeneration and for promoting neuroregeneration.
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Page/Page column 45-46

(2008/06/13)

METHOD FOR THE PRODUCTION OF LOSARTAN
The invention relates to a novel method for the production of losartan, an imidazol derivative with the chemical name 2-n-butyl-4-chloro-5-hydroxymethyl-1-{[2'-(1H-tetrazol-5-yl)biphenyl-4-]methyl}imidazol and the pharmacologically active salts thereof. The invention also relates to novel intermediate products which are suitable for the production of losartan, and to novel methods for the production of intermediate compounds which are suitable for the production of losartan. One aspect of the invention is a method for the production of a compound of general formula (I), which can arise as an intermediate step in the inventive representation of losartan.
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Page/Page column 20; 33-34

(2008/06/13)

A practical synthesis of 5-(4′-methylbiphenyl-2-yl)-1H-tetrazole
Practical synthesis of 5-(4′-methylbiphenyl-2-yl)-1H-tetrazole, key intermediate in several angiotensin II receptor antagonists from 2-fluorobenzonitrile in excellent yields and very high purity is described.
Kantevari, Srinivas,Nair, C. K. Snehalatha,Pardhasaradhi
p. 1353 - 1356
(2007/10/03)

Pyrrolidine modulators of chemokine receptor activity
The present invention is directed to pyrrolidine compounds of the formula 1: (wherein R1, R2, R3, R4, R5, R6and n are defined herein) which are useful as modulators of chemokine receptor activity. In particular, these compounds are useful as modulators of the chemokine receptors CCR-5 and/or CCR-3.
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(2008/06/13)

5-aryleheteroarylalkyl-1,3,5-trisubstituted-1,2,4-triazole compounds for treatment of circulatory disorders
A class of 5-arylheteroarylalkyl-1,3,5-trisubstituted-1,2,4-triazole compounds is described for use in treatment of circulatory disorders such as hypertension. Compounds of particular interest are angiotensin II antagonists of the formula wherein A is selected from wherein m is one; wherein R1 is selected from ethyl, n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl, tert-butyl, 4-methylbutyl, n-pentyl, neopentyl, benzyl, cyclohexyl, cyclohexylmethyl, 2-butenyl, 3-butenyl, 2-butynyl, 3-butynyl and 2-hydroxybutyl; wherein R2 is selected from ethyl, n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl, 4-methylbutyl, tert-butyl, n-pentyl, neo-pentyl, 1-oxoethyl, 1-oxopropyl, 1-oxobutyl, 1-oxopentyl, 1,1-dimethoxypropyl, 1,1-dimethoxypentyl, halo, difluoromethyl, 1-oxo-2-phenylethyl, 1-oxo-2-cyclohexylethyl, 1,1-difluoro-2-phenylethyl, 1,1-difluoro-2-cyclohexylethyl, 2-cyclohexylethyl, 1,1-difluoro-3-cyclohexylpropyl, 1,1-dimethoxybutyl, 1,1-difluoroethyl, 1,1-difluoropropyl, 1,1-difluorobutyl, 1,1-difluoropentyl, benzyl, 2-phenylethyl, 1,1-difluoro-3-phenylpropyl, cyclohexylmethyl, cyclohexanoyl, 1-butenyl, 2-butenyl, 3-butenyl, 1-butynyl, 2-butynyl, 3-butynyl, propylthio and butylthio; wherein each of R3, R4, R6 through R11 is hydrido and R5 is selected from COOH, SH, PO3H2, SO3H, CONHNH2, CONHNHSO2CF3, OH, wherein each of R42 and R43 is independently selected from chloro, cyano, nitro, trifluoromethyl, methoxycarbonyl and trifluoromethylsulfonyl.
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(2008/06/13)

N-ARYLHETEROARYLALKYL IMIDAZOL-2-ONE COMPOUNDS FOR TREATMENT OF CIRCULATORY DISORDERS
A class of N-arylheteroarylalkyl imidazol-2-one compounds is described for use in treatment of circulatory disorders such as hypertension and congestive heart failure. Compounds of particular interest are angiotensin II antagonists of the formula STR1 wherein A is selected from STR2 wherein m is one; wherein R 1 is selected from methyl, ethyl, n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl, tert-butyl, 4-methylbutyl, 2-ethylbutyl, n-pentyl, neopentyl, phenyl, methylphenyl, difluorophenyl, benzyl, phenethyl, cyclohexyl, cyclohexylmethyl, cyclohexylethyl, cyclohexanoyl, 1-oxo-2-cyclohexylethyl, benzoyl, 1-oxo-2-phenethyl, 1-oxopropyl, 1-oxobutyl, 1-oxopentyl and 2-hydroxybutyl; wherein R 0 is hydrido; wherein R 2 is selected from methyl, ethyl, n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl, tert-butyl, n-pentyl, isopentyl, neopentyl, phenyl, benzyl, phenethyl, cyclohexyl, cyclohexylmethyl, propylthio, butylthio, and hydroxyalkyl; wherein each of R 3, R 4, R 6, R 7, R. sup.8, R 9, R 10 and R. sup.11 is hydrido and R 5 must be selected from COOH, SH, P0 3 H. sub.2, SO 3 H, CONHNH 2, CONHNHSO 2 CF 3, OH, STR3 wherein each of R 42 and R 43 is independently selected from chloro, cyano, nitro, trifluoromethyl, methoxycarbonyl and trifluoromethylsulfonyl; or a tautomer thereof or a pharmaceutically-aceptable salt thereof.
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(2008/06/13)

NOVEL REAGENT FOR TETRAZOLE SYNTHESIS AND PROCESS FOR PRODUCING TETRAZOLES THEREWITH
Analkali metal azide and zinc chloride are used in combination as a tetrazole forming agent when producing 1H-tetrazoles of the formula (II): (where R is any substituent) from carbonitriles of the formula (I): R-CN(where R has the same meaning as defined above). The tetrazole forming agent permits many kinds of solvents to be used and can in principle be used with any carbonitriles. In addition, the use of inexpensive zinc chloride leads to cost reduction.
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(2008/06/13)

A Practical Synthesis of 5-Substituted Tetrazoles.
Nitrosation of N-formyl amidrazones 8a-g with sodium nitrite - aqueous hydrochloric acid gives tetrazoles 10a-g in good yields.
Boivin, Jean,Husinec, Suren,Zard, Samir Z.
p. 11737 - 11742
(2007/10/02)

METHOD OF USING 5-ARYLHETEROARYLALKYL-1,3,5-TRISUBSTITUTED-1,2,4-TRIAZOLE COMPOUNDS FOR TREATMENT OF A GLAUCOMA DISORDER
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(2008/06/13)

Pyridopyrimidine Angiotensin II Antagonists
A series of pyridopyrimidine angiotensin II (A II) antagonists was synthesized and tested for antagonism of A II. Compounds with a biphenyltetrazole pharmacophore and small alkyl groups at the 2- and 4-positions of the pyridopyrimidine ring were found to be the most potent in an AT1 receptor binding assay and in blocking the A II pressor response in anesthetized, ganglion-blocked A II-infused rats. 5,8-Dihydro-2,4-dimethyl-8--4-yl)methyl>pyridopyrimidin-7(6H)-one (4a) was one of the more potent compounds in the binding assay and was the most efficacious compound in the A II-infused rat model. Further study of 4a in Goldblatt (2K-1C) rats showed the compound to have oral bioavailability and to be an efficacious and potent compound in a high renin form of hypertension.
Ellingboe, John W.,Antane, Madelene,Nguyen, Thomas T.,Collini, Michael D.,Antane, Schuyler,et al.
p. 542 - 550
(2007/10/02)

Process for the preparation of tetrazoles
The present invention relates to a process for the preparation of 5-aryl tetrazoles of the formula: STR1 or a salt thereof comprising reacting an aryl nitrile with a trisubstituted silyl azide and a disubstituted tin oxide.
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(2008/06/13)

5-apylheteroarylalkyl-1,3,5-trisubstituted-1,2,4-triazole compounds for treatment of circulatory disorders
A class of 5-arylheteroarylalkyl-1,3,5-trisubstituted-1,2,4-triazole compounds is described for use in treatment of circulatory disorders such as hypertension. Compounds of particular interest are antiotensin II antagonists of the formula STR1 wherein A is selected from STR2 wherein m is one; wherein R1 is selected from ethyl, n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl, tert-butyl, 4-methylbutyl, n-pentyl, neopentyl, benzyl, cyclohexyl, cyclohexylmethyl, 2-butenyl, 3-butenyl, 2-butynyl, 3-butynyl and 2-hydroxybutyl; wherein R2 is selected from ethyl, n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl, 4-methylbutyl, tert-butyl, n-pentyl, neo-pentyl, 1-oxoethyl, 1-oxopropyl, 1-oxobutyl, 1-oxopentyl, 1,1-dimethoxypropyl, 1,1-dimethoxypentyl, halo, difluoromethyl, 1-oxo-2-phenylethyl, 1-oxo-2-cyclohexylethyl, 1,1-difluor-2-phenylethyl, 1,1-difluoro-2-cyclohexylethyl, 2-cyclohexylethyl, 1,1-difluoro-3-cyclohexylpropyl, 1,1-dimethoxybutyl, 1,1-difluoroethyl, 1,1-difluoropropyl, 1,1-difluorobutyl, 1,1-difluoropentyl, benzyl, 2-phenylethyl, 1,1-difluoro-3-phenylpropyl, cyclohexylmethyl, cyclohexanoyl, 1-butenyl, 2-butenyl, 3-butenyl, 1-butynyl, 2-butynyl, 3-butynyl, propylthio and butylthio; wherein each of R3, R4, R6 through R11 is hydrido and R5 is selected from COOH, SH, PO3 H2, SO3 H, CONHNH2, CONHNHSO2 CF3, OH, STR3 wherein each of R42 and R43 is independently selected from chloro, cyano, nitro, trifluoromethyl, methoxycarbonyl and trifluoromethylsulfonyl.
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(2008/06/13)

Dialkyltin Oxide Mediated Addition of Trimethylsilyl Azide to Nitriles. A Novel Preparation of 5-Substituted Tetrazoles
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Wittenberger, Steven J.,Donner, B. Gregory
p. 4139 - 4141
(2007/10/02)

SUBSTITUTED PYRROLOPYRIMIDINES, AZEPINOPYRIMIDINES AND PYRIDOPYRIMIDINES USEFUL AS ANGIOTENSIN II ANTAGONISTS
This invention relates to pyrrolo-, pyrido-, azepino-, and azocinopyrimidines of the general formula I STR1 wherein R 1, R. sup.2, R 3, and R 4 are independently H, lower alkyl containing 1 to 6 carbon atoms, or perfluoroalkyl containing 1 to 6 carbon atoms; R. sup.5 is H or when n is 1 R 5 taken together with R 3 comprises a double bond; n is 0 to 1; p is 0 to 2; m is 0 to 3; Ar 1 is STR2 wherein W is H, lower alkyl containing 1 to 6 carbon atoms, halogen, hydroxy, or lower alkoxy containing 1 to 6 carbon atoms; Ar 2 is STR3 wherein X is STR4 wherein R. sup.6 is H, tert-butyl, tri-n-butylstannyl, or triphenylmethyl; and the pharmaceutically acceptable salts thereof which by virtue of their ability to antagonize angiotensin II are useful for the treatment of hypertension, congestive heart failure, and restenosis. The compounds are also useful for reducing lipid levels in the blood plasma and are thus useful for treating hyperlipidemia and hypercholesterolemia. Also disclosed are processes for the production of said compounds and pharmaceutical compositions containing said compounds.
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(2008/06/13)

SUBSTITUTED PYRRIDOPYRIMIDINES USEFUL AS ANGIOTENSIN II ANTAGONISTS
This invention relates to pyrrolo-, pyrido-, azepino-, and azocinopyrimidines of the general formula I STR1 useful for treating hypertension and congestive heart failure, to pharmaceutical compositions, and to methods for production thereof.
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(2008/06/13)

Directed metalation and new synthetic transformations of 5-aryltetrazoles
The tetrazole moiety is a useful directing group for the lithiation of 5-aryl substituents. Dilithiated 5-aryltetrazoles generally react with alkyl halides and aldehydes to give substitution and addition products, respectively.
Flippin, Lee A.
p. 6857 - 6860
(2007/10/02)