cas 19355-69-2, 2-AMINO-2-METHYL-PROPIONITRILE

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Taillades,Commeyras
p. 3407,3409, 3411
(1974)
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Photoreactive fused aziridinylpiperazines on the background of 4-substituted chalcones and their benzimidazolic analogs
The reaction of bromo-substituted chalcones with various diamino-compounds leads to the fused heterocyclic products, aziridinylpiperazines, exhibiting photoreactivity in the crystalline state. Crystals of 4-nitrosubstituted compounds of this family change their color from yellowish to deep violet-blue, 4-cyanosubstituted ones – from yellowish to pink at UV irradiation. Discussion on the mechanism of this phototransformation is still in progress, however, several facts points to the free radial nature of the photogenerated colored semi-products stabilized only by crystalline state of the irradiated samples. Formation of a mixture of positional isomers at interaction of bromo-chalcones with asymmetric diamines of aliphatic/alicyclic or aromatic series at synthesis of the title compounds is of significant interest as well.
Kotlyar, Volodymyr M.,Kolomoitsev, Oleksii O.,Nikolaievskyi, Dmytro V.,Pedan, Polina I.,Chumak, Andrii Yu,Orlov, Valery D.,Shishkina, Svitlana V.,Doroshenko, Andrey O.
p. 741 - 746
(2019/01/10)

Preparation method of enzalutamide intermediate
The invention discloses a preparation method of an enzalutamide intermediate and belongs to the field of pharmaceutical and chemical industry. According to the preparation method of the enzalutamide intermediate, the reaction of every process is high up to higher than 80%, certain reaches up to 93%. Meanwhile, the preparation method of the enzalutamide intermediate is simple in aftertreatment process, easy to operate and applicable to industrializing, mild in reaction conditions and free from severe reaction conditions of high temperature, high pressure and ultralow temperature.
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Paragraph 0025; 0033; 0034

(2018/08/28)

METHOD FOR PRODUCING ALPHA-HYDROXY CARBOXYLIC ESTERS IN THE GAS PHASE
The present invention relates to a process for preparing alpha-hydroxycarboxylic esters from the alcoholysis of alpha-hydroxycarboxam ides in the gas phase, characterized in that the conversion is effected in the presence of water.
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Paragraph 0049-0050

(2017/06/23)

Prebiotic selection and assembly of proteinogenic amino acids and natural nucleotides from complex mixtures
A central problem for the prebiotic synthesis of biological amino acids and nucleotides is to avoid the concomitant synthesis of undesired or irrelevant by-products. Additionally, multistep pathways require mechanisms that enable the sequential addition of reactants and purification of intermediates that are consistent with reasonable geochemical scenarios. Here, we show that 2-aminothiazole reacts selectively with two- and three-carbon sugars (glycolaldehyde and glyceraldehyde, respectively), which results in their accumulation and purification as stable crystalline aminals. This permits ribonucleotide synthesis, even from complex sugar mixtures. Remarkably, aminal formation also overcomes the thermodynamically favoured isomerization of glyceraldehyde into dihydroxyacetone because only the aminal of glyceraldehyde separates from the equilibrating mixture. Finally, we show that aminal formation provides a novel pathway to amino acids that avoids the synthesis of the non-proteinogenic α,α-disubstituted analogues. The common physicochemical mechanism that controls the proteinogenic amino acid and ribonucleotide assembly from prebiotic mixtures suggests that these essential classes of metabolite had a unified chemical origin.
Islam, Saidul,Bu?ar, Dejan-Kre?imir,Powner, Matthew W.
p. 584 - 589
(2017/05/31)

PYRAZOLYL AMIDE COMPOUNDS AND USES THEREOF
Disclosed is a pyrazole amide compound of a novel structure as represented by general formula I, wherein, each substituent group is as defined in the specification. The compound of general formula I has good insecticidal activity, and can be used for pest control.
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Paragraph 0096-0098

(2016/10/27)

NON-STEROIDAL ANTIANDROGENS AND SELECTIVE ANDROGEN RECEPTOR MODULATORS WITH A PYRIDYL MOIETY
Compounds having the structure or their salts: are used to treat or reduce the likelihood of acquiring androgen-dependent diseases, such as prostate cancer, benign prostatic hyperplasia, polycystic ovarian syndrome, acne, hirsutism, seborrhea, androgenic alopecia, male baldness, muscle atrophy and weakness, sarcopenia, male hypogonadism, erectile dysfunction, female sexual dysfunction and osteoporosis. They can be formulated together with pharmaceutically acceptable diluent or carrier or otherwise made into any pharmaceutical dosage form. Combinations with other active pharmaceutical agents are also disclosed.
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Paragraph 0173; 0174

(2015/07/02)

THERAPEUTICALLY ACTIVE COMPOUNDS AND THEIR METHODS OF USE
Provided are compounds useful for treating cancer and methods of treating cancer comprising administering to a subject in need thereof a compound described herein.
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Page/Page column 149

(2015/02/02)

Transamination of a-amino nitriles
α-Amino nitriles containing a primary amino group undergo transamination with aliphatic and aromatic amines under mild conditions with high yields. A probable reaction mechanism involving intermediate elimination of cyanide ion has been proposed.
Popov,Mokhov,Tankabekyan
p. 21 - 24
(2014/03/21)

Structural modifications of 5,6-dihydroxypyrimidines with anti-HIV activity
A series of 5,6-dihydroxypyrimidine analogs were synthesized and evaluated for their anti-HIV activity in vitro. Among all of the analogs, several compounds exhibited significant anti-HIV activity, especially 1b and 1e, which showed the most potent anti-HIV activity with EC50 values of 0.14 and 0.15 μM, and TI (therapeutic index) values of >300 and >900, respectively. Further docking studies revealed that the representative compounds 1e and 3a could meet the HIV-1 integrase inhibition minimal requirements of a chelating domain (two metal ions) and an aromatic domain (π-π stacking interactions).
Guo, Di-Liang,Zhang, Xing-Jie,Wang, Rui-Rui,Zhou, Yu,Li, Zeng,Xu, Jin-Yi,Chen, Kai-Xian,Zheng, Yong-Tang,Liu, Hong
supporting information
p. 7114 - 7118
(2013/01/15)

Identification, synthesis, and strategy for minimization of potential impurities observed in raltegravir potassium drug substance
Multiple sources of anticipated degradation and process impurities of raltegravir potassium drug substance observed during the laboratory optimization and later during its bulk synthesis are described in this article. The impurities were monitored by UPLC, and their structures are tentatively assigned on the basis of fragmentation patterns in LC-MS and NMR spectroscopy. Most of the impurities are synthesized, and their assigned constitutions were confirmed by co-injection in UPLC. In addition to the formation, synthesis, and characterization, strategy for minimizing these impurities to the level accepted by ICH is also described. We feel that our study will be helpful to the generic industry for obtaining chemically pure raltegravir potassium.
Patil, Gulabrao D.,Kshirsagar, Siddheshwar W.,Shinde, Shivnath B.,Patil, Pankaj S.,Deshpande, Mangesh S.,Chaudhari, Ashok T.,Sonawane, Swapnil P.,Maikap, Golak C.,Gurjar, Mukund K.
p. 1422 - 1429
(2012/10/29)

TOPP: A novel nitroxide-labeled amino acid for EPR distance measurements
A new tool: The amino acid 4-(3,3,5,5-tetramethyl-2,6-dioxo-4- oxylpiperazin-1-yl)-L-phenylglycine (TOPP), which has a rigid nitroxide spin label, can be used for EPR-based distance measurements in peptides. The key feature of the design is the defined orientation of the nitroxide in space with respect to the peptide backbone. EPR measurements provide evidence for the low conformational flexibility of the TOPP label. Copyright
Stoller, Sven,Sicoli, Giuseppe,Baranova, Tatiana Y.,Bennati, Marina,Diederichsen, Ulf
supporting information; experimental part
p. 9743 - 9746
(2011/11/29)

Development of a second-generation, highly efficient manufacturing route for the HIV integrase inhibitor raltegravir potassium
A manufacturing route for the synthesis of raltegravir potassium 1 was developed via a thermal rearrangement of amidoxime DMAD adducts 6 to construct the key, highly functionalized hydroxypyrimidinone core 7. Utilizing this route 1 was prepared in nine linear chemical steps with 22% overall yield. A second-generation synthesis was subsequently developed that solved the key chemical, productivity, and environmental impact issues of the initial synthesis. Highlights of the new synthesis include a highly selective methylation, 3-4-fold higher productivity, and a 65% reduction of combined organic and aqueous waste produced. The efficient second-generation manufacturing route provides raltegravir potassium 1 in 35% overall yield.
Humphrey, Guy R.,Pye, Philip J.,Zhong, Yong-Li,Angelaud, Remy,Belyk, Kevin M.,Maligres, Peter E.,Miller, Ross A.,Reamer, Robert A.,Askin, David,Mancheno, Danny E.,Weissman, Steven A.
experimental part
p. 73 - 83
(2011/09/16)

Design and synthesis of dipeptidyl nitriles as potent, selective, and reversible inhibitors of cathepsin C
A series of dipeptide nitriles with a thienyl alanine in P2 were identified as potent and selective cathepsin C inhibitors. Incorporation of a substituted cyclopropyl moiety in P1 effectively protects these derivatives against hydrolase activity in whole blood.
Guay, Daniel,Beaulieu, Christian,Jagadeeswar Reddy,Zamboni, Robert,Methot, Nathalie,Rubin, Joel,Ethier, Diane,David Percival
scheme or table
p. 5392 - 5396
(2010/05/02)

Versatile synthesis of free and N-benzyloxycarbonyl-protected 2,2-disubstituted taurines
An effective and versatile method was developed to synthesize N-benzyloxycarbonyl-protected and free 2,2-disubstituted taurines. Several novel 2,2-disubstituted taurines, including aliphatic/aromatic and cyclic/acyclic derivatives, were obtained, which demonstrates the generality of this method. Wiley-VCH Verlag GmbH & Co. KGaA, 2008.
Wang, Boyuan,Zhang, Wei,Zhang, Leilei,Du, Da-Ming,Liu, Gang,Xu, Jiaxi
p. 350 - 355
(2008/09/18)

TASTE-MASKED TABLETS AND GRANULES
Orally administered, taste-masked tablets and granules contain (a) a hydroxypyrimidinone carboxamide, a hydroxy-tetrahydropyridopyrimidinone carboxamide, or a related carboxamide compound, or a pharmaceutically acceptable salt thereof, (b) a taste-masking polymer, (c) a superdisintegrant, and optionally other excipients. The carboxamide compound is an HIV integrase inhibitor, and the tablets and granules are suitable for use in the inhibition of HIV integrase, the treatment or prophylaxis of HIV infection, and the treatment or prophylaxis or delay in the onset of AIDS.
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Page/Page column 29-30

(2008/06/13)

Methods and compositions for treating amyloid-related diseases
Methods, compounds, pharmaceutical compositions and kits are described for treating or preventing amyloid-related disease.
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Page/Page column 157

(2010/11/24)

Helix 12 directed non-steroidal antiandrogens
Compounds having the structure (or their salts): are used to treat or reduce the likelihood of acquiring androgen-dependent diseases, such as prostate cancer, benign prostatic hyperplasia, polycystic ovarian syndrome, acne, hirsutism, seborrhea, androgenic alopecia and male baldness. The compounds can be formulated together with pharmaceutically acceptable diluents or carriers or otherwise made into any pharmaceutical dosage form. Combinations with other active pharmaceutical agents are also disclosed.
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Page/Page column 53

(2010/11/25)

Potassium salt of an HIV integrase inhibitor
Potassium salts of Compound A and methods for their preparation are disclosed, wherein Compound A is of formula: Compound A is an HIV integrase inhibitor useful for treating or prophylaxis of HIV infection, for delaying the onset of AIDS, and for treating or prophylaxis of AIDS.
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Page/Page column 21

(2010/11/08)

USE OF ATAZANAVIR FOR IMPROVING THE PHARMACOKINETICS OF DRUGS METABOLIZED BY UGT1A1
A method for improving the pharmacokinetics of an orally administered drug that is directly metabolized by UGT1A1 comprises orally administering to a mammal in need of treatment with the drug a combination of the drug or a pharmaceutically acceptable salt thereof and atazanavir or a pharmaceutically acceptable salt thereof.
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Page/Page column 27-28

(2010/11/08)

PHARMACEUTICAL COMPOSITION CONTAINING AN ANTI-NUCLEATING AGENT
Pharmaceutical compositions suitable for oral administration in solid dosage forms are described. The compositions comprise an effective amount of a drug compound in the form of a salt, wherein the drug salt is characterized by conversion to a less soluble form of the drug compound under certain pH conditions, and an anti-nucleating agent.
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Page/Page column 27

(2010/11/08)

PHARMACEUTICAL FORMULATION CONTAINING A RELEASE RATE CONTROLLING COMPOSITION
Pharmaceutical formulations suitable for oral administration in solid dosage forms are described. The compositions comprise an effective amount of a base salt of a compound of Formula (I) and a release rate controlling composition comprising a solubilizing agent, a gelling agent, and a water soluble filler; wherein R1, R2, R3 and R4 are defined herein. The formulations are suitable for use in the inhibition of HIV integrase, the treatment and prophylaxis of HIV infection, and the treatment, prophylaxis and delay in the onset of AIDS.
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Page/Page column 22-23

(2010/11/08)

CATHEPSIN INHIBITORS
This invention relates to a novel class of compounds, represented by the formula (I) below, wherein the meanings of R1, R2, R3 and R4 are indicated therein, which are cysteine protease inhibitors, including but not limited to, inhibitors of cathepsins K, L, S and B. These compounds are useful for treating diseases in which inhibition of bone resorption is indicated, such as osteoporosis, osteoarthritis and rheumatoid arthritis.
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Page/Page column 64-65

(2010/02/11)

Studies on phosphoroheterocycle chemistry II: A simple and new route to 1,3,2-diazaphospholidine-4-thione 2-sulfide derivatives
A simple and new method for the synthesis of phosphoroheterocycles 1,3,2-diazaphospholidine-4-thione 2-sulfide derivatives by treatment of Lawesson's reagent (LR) with a variety of α-aminonitriles has been developed. The same methodology was also used in the preparation of fused phosphoroheterocycle 6 from 5-amino-4-cyano-3-methylthia-l-phenylpyrazole. The possible mechanism of the reaction involving addition of P-SH to the nitrile and subsequent rearrangement is proposed.
Deng,Liu
p. 2445 - 2449
(2007/10/03)

Regioselectivity of the photochemical addition of ammonia, phosphine, and silane to olefinic and acetylenic nitriles
An investigation of the regioselectivity and mechanisms of the photochemical addition of NH3, PH3, and SiH4 to olefinic and acetylenic nitriles is described. The photolysis of NH3 in the presence of acrylonitrile led to the α-addition product 2-aminopropanenitrile (2), propanenitrile, and 2,3-dimethylbutanedinitrile (3). When NH3 was photolyzed in the presence of substituted derivatives (crotononitrile, methacrylonitrile, or 1-cyclohexenecarbonitrile), the α-addition products were still obtained. However, under similar reaction conditions, only the β-addition products, 7 and 8, were obtained from acrylonitrile and PH3, or acrylonitrile and SiH4, respectively. On the other hand, the photolysis of 2-butynenitrile and NH3 gave the β-addition products, (Z)- and (E)-3-aminocrotononitrile (10). The photolysis of these acetylenic nitriles with PH3 or SiH4 also gave the β-adducts (12) and (13). The α-addition of NH3 proceeds by the stepwise addition of H· and ·NH2, respectively, to the α,β-unsaturated nitriles. The β-addition products are formed by a radical chain mechanism initiated by photochemically generated radicals. The radical chain pathway provides an explanation for a number of previously described photochemical additions to olefins and acetylenes. Photochemical processes similar to the addition of ammonia and phosphine to unsaturated organic compounds may have played a role in the evolution of the atmosphere of the primitive Earth, and may even be currently occurring in the atmospheres of other planets.
Guillemin, Jean-Claude,Breneman, Curt M.,Joseph, Jeffrey C.,Ferris, James P.
p. 1074 - 1082
(2007/10/03)

Studies into the synthesis of derivatives of 4-amino-2,3-dihydroisothiazole 1,1-dioxides and 4-amino-1,2-oxathiole 2,2-dioxides, the search for linked π-system containing analogues as potential inhibitors of HIV-1 reverse transcriptase
The synthesis, and anti HIV-1 activity, of new derivatives of 4-amino-1,2-oxathiole 2,2-dioxide (3, 5, 6 and 9) and 4-amino-2,3-dihydroisothiazole 1,1-dioxide (14), a new heterocyclic ring system, is described.
Ingate, Simon T.,Marco, Jose L.,Witvrouw, Myriam,Pannecouque, Cristophe,De Clercq, Erik
p. 17795 - 17814
(2007/10/03)

α-Aminonitrile hydration in the presence of hydrogen peroxide in aqueous basic medium
α-Aminonitriles are hydrated into α-aminoamides in the presence of hydrogen peroxide in sodic or ammoniacal basic medium. While the hydration mechanism is close to the mechanism described previously in the case of aromatic nitrites, we showed that, in weakly basic conditions, the amine function of α-aminonitrile is competitively oxidized via a peroxyimidic acid by an intramolecular process. In the case of 2-aminopropanenitrile, this reaction leads to pyruvamide oxime. Furthermore, the study of structurereactivity relationships in the hydration of aliphatic and aromatic monofunctional nitriles and α-aminonitriles showed that the reactivity of the substrates towards hydroperoxide onion, which mostly depends on inductive effects of the substituents, is sufficiently enhanced to allow hydration of tertiary α-aminonitriles with low steric hindrance and regioselective hydration of dissymmetric α-aminodinitriles. Eisevier,.
Taillades, Jacques
p. 89 - 100
(2007/10/03)

Inhibitors of acyl-CoA:cholesterol O-acyl transferase (ACAT) as hypocholesterolemic agents. 8. Incorporation of amide or amine functionalities into a series of disubstituted ureas and carbamates. Effects of ACAT inhibition in vitro and efficacy in vivo
A series of disubstituted ureas containing amide or amine groups was prepared and evaluated for their ability to inhibit acyl-CoA:cholesterol O- acyl transferase in vitro and to lower plasma total cholesterol in a variety of cholesterol-fed rat models in vivo. The presence of polar or ionizable functionalities within this class of compounds may impart greater aqueous solubility to those compounds and thus allow improved transport to the enzyme location within the intestinal enterocyte. Compounds from this class exhibit good cholesterol lowering in a chronic cholesterol-fed rat model of hypercholesterolemia even when dosed in an aqueous vehicle. In general, the amine-containing compounds were more potent and efficacious than the amides in the acute rat model of hypercholesterolemia. Further structure-activity relationship studies showed that the preferred position of the amide/amine group was β to the urea moiety and not α, and that in this series, the presence of a secondary amine (or amide) proton is required for good in vitro potency. One of these compounds, 9n(-), lowered plasma total cholesterol (- 47%) and elevated high-density lipoprotein cholesterol (+256%) when dosed in an aqueous vehicle to rats with preestablished hypercholesterolemia.
O'Brien,Sliskovic,Blankley,Roth,Wilson,Hamelehle,Krause,Stanfield
p. 1810 - 1822
(2007/10/02)

N-cyanoalkyl-N-haloalkylthio carboxamides as fungicides
N-cyanoalkyl-N-haloalkylthio alkyl-, aryl- and aralkyl-carboxamides of the general formula: STR1 wherein R is alkyl of 1 to 10 carbon atoms, cycloalkyl of 3 to 10 carbon atoms, lower alkenyl of 2 to 6 carbon atoms or lower alkynyl of 2 to 6 carbon atoms, all optionally substituted with 1 to 4 halogen atoms; lower alkoxyalkylene; aryl of 6 to 12 carbon atoms; aralkyl of 7 to 16 carbon atoms; or substituted aryl or substituted aralkyl both substituted with 1 to 3 substituents independently selected from phenyl, lower alkyl of 1 to 6 carbon atoms, lower alkoxy of 1 to 6 carbon atoms, lower alkylthio of 1 to 6 carbon atoms, halogen, nitro, cyano, STR2 wherein R4 is hydrogen or lower alkyl of 1 to 6 carbon atoms, STR3 wherein R5 and R6 are independently hydrogen or lower alkyl of 1 to 6 carbon atoms; R1 and R2 are independently hydrogen, or lower alkyl of 1 to 6 carbon atoms; and R3 is alkyl of 1 to 3 carbon atoms substituted with 3 to 6 halogen atoms or trihalovinyl are fungicidal.
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(2008/06/13)

Fungicidal N-cyanoalkyl-N-haloalkylthio sulfonamides
Compounds of the formula: STR1 wherein R is aryl of 6 to 12 carbon atoms or aralkyl of 7 to 14 carbon atoms either optionally substituted with 1 to 3 substituents independently selected from lower alkyl of 1 to 6 carbon atoms, lower alkoxy of 1 to 6 carbon atoms, lower alkylthio of 1 to 6 carbon atoms, lower alkylsulfinyl of 1 to 6 carbon atoms, lower alkylsulfonyl of 1 to 6 carbon atoms, halogen, trihalomethyl, nitro, cyano or carboxyl; alkyl of 1 to 10 carbon atoms, cycloalkyl of 3 to 10 carbon atoms, lower alkenyl of 2 to 6 carbon atoms, or lower alkynyl of 2 to 6 carbon atoms, all optionally substituted with 1 to 3 halogen atoms; lower alkoxyalkylene; lower alkylene carbalkoxy; lower alkylthioalkylene; lower alkylsulfinylalkylene; or lower alkylsulfonylalkylene; R1 and R2 are independently hydrogen, lower alkyl of 1 to 6 carbon atoms, aryl of 6 to 12 carbon atoms, or thienyl, or taken together form an alkylene bridge to give a cycloalkyl group of 3 to 10 carbon atoms; and R3 is alkyl of 1 to 3 carbon atoms substituted with 3 to 6 halogen atoms or trihalovinyl are fungicidal.
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(2008/06/13)

Synthesis of 4,4-Disubstituted 1,3-Thiazol-5(4H)-thiones
An easy synthesis for the 1,3-thiazol-5(4H)-thiones 5, a class of heterocycles which have hitherto only been available with difficulty, is described.Reaction of 3-amino-2H-azirines 25 with thiocarboxylic acids at 0 deg yields monothiodiamides of type 20 (Scheme 6) which, on treatment with Lawesson reagent at 100 deg, undergo thiation and cyclization to give 5 in good yield.
Jenny, Christjohannes,Heimgartner, Heinz
p. 374 - 388
(2007/10/02)

Systemes de Strecker et apparentes XV. Comportement d'α-alcoylaminonitriles en presence de CS2 et de CO2
Dans le cadre de l'etude de la reaction de Bucherer-Bergs (transformation, en solution aqueuse, d'un compose carbonyle en acide α-amine correspondant via l'α-aminonitrile puis l'imidazolidinedione-2,4) le comportement d'α-alcoylaminonitriles en presence de CS2 est examine et elargi au systeme α-alcoylaminonitriles/CO2 en solution aqueuse.En presence de CS2, l'α-aminonitrile conduit a la formation equilibree d'imino-5 thiazolidine thione-2.Son evolution ulterieure vers l'imidazolidine dithione-2,4 alcoyle-1 est bloquee par la substitution sur l'azote 3.Par contre, nous avons mis en evidence la formation inattendue de l'imidazolidine dithione-2,4 non substituee.En solution aqueuse et en presence de CO2, l'imino-5 oxazolidinone-2 que nous n'avons pas decelee doit etre en equilibre tres defavorise avec l'α-carboxyaminonitrile.Les seules reactions observees sont l'hydratation autocatalitique de l'α-aminonitrile et sa decomposition en hydroxy-2 propionitrile et en α-aminodinitrile.
Rousset, A.,Lasperas, M.,Taillades, J.,Commeyras, A.
p. 209 - 216
(2007/10/02)

Process for the preparation of azo compounds from amino compounds in the presence of a phase transfer catalyst
Azo compounds of the formula, STR1 wherein each of R1 and R2 is selected from the group consisting of (1) C1 -C8 aliphatic hydrocarbons unsubstituted or substituted with carboxyl, hydroxyl or alkoxy of the formula --OR4 in which R4 is a C1 -C4 aliphatic hydrocarbon, (2) C3 -C8 alicyclic hydrocarbons, (3) C6 -C10 aromatic hydrocarbons and (4) C4 -C12 alicyclic hydrocarbons formed by combining R1 and R2 together with the adjacent carbon atom, and R3 is selected from the group consisting of nitrile, esters of the formula --COOR4 in which R4 is a C1 -C4 aliphatic hydrocarbon, a carboxylate of the formula --COOM in which M is an alkali metal or alkaline earth metal, and a carboxylamido, which are useful as foaming agents or radical polymerization initiator, are prepared in a high yield by reacting a corresponding amino compound with a metal hypohalite or with an alkyl hypohalite in the presence of an alkali, using a phase transfer catalyst in a heterogeneous medium comprising water and organic solvent, the phase transfer catalyst being one member selected from the group consisting of organic quaternary ammonium salts, organic quaternary phosphonium salts and macrocyclic polyethers.
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(2008/06/13)

Preparation of 2,2'-azobis(2-methylpropionitrile)
2,2'-Azobis(2-methylpropionitrile), which is used as a foaming agent and a radical polymerization initiator, is produced in a high yield and a high purity, by (1) subjecting a crude 2-amino-2-methylpropionitrile product obtained by the reaction between acetone cyanohydrin and ammonia, to reduced pressure distillation, (2) contacting the resulting purified 2-amino-2-methylpropionitrile product having an ammonia content of 1.5% by weight or less with an aqueous metal hypochlorite solution, and then (3) treating the resulting aqueous suspension of 2,2'-azobis(2-methylpropionitrile) with a reducing agent.
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(2008/06/13)

Ureidonitriles useful as antihypertensives
Ureidonitriles, such as N-(1-cyano-1-methylethyl)-N'-(1,1-dimethylethyl)urea with antihypertensive activity in warm-blooded animals.
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(2008/06/13)

Herbicidal 5-pyrimidinecarbonitriles
5-Pyrimidinecarbonitriles, having amino substituents in the 2 and 6 positions and an alkoxy substituent in the 4 position, exhibit herbicidal activity. The preparation of novel active compounds and intermediates in this class is described; herbicidal compositions containing the active compounds are illustrated; and methods for utilizing the herbicidal compositions to control plant growth are disclosed.
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(2008/06/13)

Cyclopenta[c]pyrrole derivatives
2,4,5,6-Tetrahydrocyclopenta[c]pyrrole-4-carboxamide and 4-thiocarboxamide derivatives useful as anti-secretory and anti-ulcer agents are prepared by hydrolysis or thiohydrolysis of the corresponding 2,4,5,6-tetrahydrocyclopenta[c]pyrrole-4-carbonitriles or, in the case of the thiocarboxamides, by reaction of the 4-carboxamide with phosphorus pentasulfide.
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(2008/06/13)

Water-soluble amine-linked polymeric colorants
Polymeric colorants comprising a hydrocarbon backbone and attached directly thereto through amine linkages, at least one water-solubilizing group and at least one optically chromophoric group are disclosed. In a preferred embodiment, the backbone is a saturated aliphatic hydrocarbon, the chromophore is an anthraquinone chromophore and the solubilizing group is a sulfonate or sulfamate residue.
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(2008/06/13)