- Preparation method of 2-chloro-N, N-dimethyl nicotinamide
-
The invention belongs to the technical field of pesticides, and particularly relates to a preparation method of 2-chloro-N, N-dimethyl nicotinamide. The preparation method of the 2-chloro-N, N-dimethyl nicotinamide comprises the following steps of taking 2-chloronicotinic acid as a raw material, and carrying out esterification reaction with methanol to obtain 2-chloronicotinic acid methyl ester, and carrying out aminolysis reaction with dimethylamine in the presence of a catalyst N, N-dimethyl nicotinamide to obtain the 2-chloro-N, N-dimethyl nicotinamide. The preparation method disclosed by the invention is mild and controllable in reaction, simple in process equipment, low in dimethylamine consumption, low in production cost and good in product quality, and the amount of wastewater is greatly reduced and is easy to treat.
- -
-
Paragraph 0010; 0025-0026; 0028-0029; 0031-0032
(2021/03/13)
-
- LIBRARIES OF PYRIDINE-CONTAINING MACROCYCLIC COMPOUNDS AND METHODS OF MAKING AND USING THE SAME
-
The present disclosure relates to novel pyridine-containing macrocyclic compounds and libraries thereof that are useful as research tools for drug discovery efforts. This disclosure also relates to methods of preparing these compounds and libraries and methods of using these libraries, such as in high throughput screening. In particular, these libraries are useful for evaluation of bioactivity at existing and newly identified pharmacologically relevant targets, including G protein-coupled receptors, nuclear receptors, enzymes, ion channels, transporters, transcription factors, protein-protein interactions and nucleic acid-protein interactions. As such, these libraries can be applied to the search for new pharmaceutical agents for the treatment and prevention of a range of medical conditions.
- -
-
Paragraph 00221
(2019/01/11)
-
- A ultrasonic process for synthesizing 2 - halogenated nicotinate and intermediates thereof
-
The invention discloses a method for synthesizing 2-halogenated ester nicotinate and a 2-halogenated ester nicotinate intermediate according to an ultrasonic method. The method comprises the following steps: adding substituent amino acrolein, a catalyst and cyanacetic ester into a reactor for a reaction under ultrasonic radiation; tracing the reaction till substituent amino acrolein is disappeared, thereby obtaining a reaction solution I containing the 2-halogenated ester nicotinate intermediate; then, adding halogen hydride into the reaction solution I for another reaction to obtain a reaction solution II; tracing and monitoring the reaction till completion; adding a lye into the reaction solution II to adjust the pH value of the reaction solution II to be 5-6; carrying out standing stratification to obtain a water layer and an organic layer; conducting extraction on the water layer by utilizing an organic solvent, and then combining the extraction solution with the organic layer; carrying out refining to obtain 2-halogenated ester nicotinate. Through the adoption of the method, an organic synthesis reaction can be effectively facilitated, the reaction speed and yield can be improved, and the environmental protection can be promoted; the reaction time is short and the operation is simple, that is, the organic synthesis reaction can be finished within 2 hours in general; the product yield and quality are high; specifically, the product yield can reach 90% or higher, and exceed that achieved according to the conventional solvent heating reflux method.
- -
-
Paragraph 0057; 0058; 0061
(2018/04/21)
-
- A microwave synthesis 2 - halogenated nicotinate and intermediates thereof
-
The invention discloses a method for synthesizing 2-halogenated nicotinic acid ester and intermediates thereof through microwave method. The method comprises the following steps: adding substitute amino acrolein, a catalyst and cyan-acetic ester into a reactor, carrying out reaction under microwave radiation, and tracking the reaction till substitute amino acrolein disappears to prepare and obtain reaction liquid of the intermediates of 2-halogenated nicotinic acid ester; adding hydrogen halide into the reaction liquid, continuously carrying out reaction, and tracking and monitoring the reaction till the reaction is complete; adding alkali liquor into the reaction liquid to adjust the pH value to 5-6; carrying out standing delamination to obtain an aqueous layer and an organic layer; extracting the aqueous layer with an organic solvent, combining the extracted aqueous layer with the organic layer, and carrying out refinement to prepare and obtain 2-halogenated nicotinic acid ester. The synthesis method of 2-halogenated nicotinic acid ester related to the invention has the advantages of beingenvironment-friendly, short in reaction time, simple to operate, high in product yield and good in quality.
- -
-
Paragraph 0034; 0035
(2018/05/16)
-
- Towards new sila- Or germa-derivatives of motesanib
-
– Developing new access to original silylated heterocycles is an emerging challenge in medicinal chemistry. In this paper, we describe a synthesis of silylated and germylated Motesanib analogues relying on a peptide coupling between a nicotinic acid derivative and silylated or germylated heterocycles, prepared according to our previous reports.
- Boddaert, Thomas,Querolle, Olivier,Meerpoel, Lieven,Angibaud, Patrick,Maddaluno, Jacques,Durandetti, Muriel
-
p. 1210 - 1218
(2019/07/31)
-
- A fluorine-containing tetrazine pyridine compound and its use
-
The invention provides fluorine-containing tetrazine pyridine compounds disclosed as Formula I. The compounds have ultrahigh inhibiting and killing actions on harmful acarids and acarid ova, and can be used as an acaricide for controlling acarid harm in agriculture and forestry.
- -
-
Paragraph 0010; 0029; 0030
(2017/08/25)
-
- Method using hydrothermal method to synthesize 2-halogeneated nicotinate and 2-halogeneated nicotinic acid
-
The invention discloses a method using a hydrothermal method to synthesize 2-halogeneated nicotinate and 2-halogeneated nicotinic acid and relates to the field of chemical synthesizing. The method uses substituted amino acrolein, catalyst, catalyst assistant, water and cyanoacetate as raw materials to synthesize the 2-halogeneated nicotinate and the 2-halogeneated nicotinic acid through the hydrothermal method. Compared with the prior art, the method is environmentally friendly, easy in separation, high in product yield, good in product quality, capable of achieving large-scale industrial production favorably, and the like.
- -
-
Paragraph 0031; 0032
(2017/11/01)
-
- An ionic liquid method of synthesizing 2 - halogenated nicotinate and intermediates thereof
-
The invention discloses a method for synthesizing 2-halogenated nicotinate and an intermediate thereof through an ionic liquid method. The method comprises the steps that cyan-acetic ester, ionic liquid and substituted amino acrolein are evenly mixed and heated to a preset temperature for conducting a reaction, the reaction is tracked till the substituted amino acrolein disappears, reaction liquid is cooled to the room temperature and extracted for multiple times through organic solvents, the residual phase of the ionic liquid is reused after being washed and dried, and the intermediate of the 2-halogenated nicotinate is obtained by evaporating the organic solvents from the organic phase; when the 2-halogenated nicotinate is synthesized, the organic solvents do not need to be separated from the intermediate of the 2-halogenated nicotinate, the reaction is continuously conducted by adding hydrogen halide into the organic phase, and the tracking monitoring is conducted till the reaction is completed; the 2-halogenated nicotinate product is prepared after separation. The synthesizing method of the 2-halogenated nicotinate has the advantages of being green and environmentally friendly, easy to operate, high in product yield and good in quality of the synthesized product.
- -
-
Paragraph 0060; 0061; 0062
(2017/10/13)
-
- RING-FUSED 2-PYRIDONE DERIVATIVES AND HERBICIDES
-
Provided are 2-pyridone derivatives which have excellent herbicidal activity and exhibit high safety to useful crops and so on; salts thereof; and herbicides containing same. In more detail, 2-pyridone derivatives represented by general formula [I] or agrochemically acceptable salts thereof, and herbicides containing these compounds are provided. In general formula [I], X1 is an oxygen atom or a sulfur atom; X2, X3, and X4 are to each CH or N(O)m; m is an integer of 0 or 1; R1 is a hydrogen atom, a C1-12 alkyl group, or the like; R2 is a halogen atom, a cyano group, or the like; n is an integer of 0 to 4; R3 is a hydroxyl group, a halogen atom, or the like; A1 is C(R11R12); A2 is C(R13R14) or C═O; A3 is C(R15R16); and R11, R12, R13, R14, R15, and R16 are each independently a hydrogen atom or a C1-6 alkyl group.
- -
-
Page/Page column 72-73
(2011/12/12)
-
- Claisen condensation of N-methylpyrrolidinone and α-chloronicotinic esters
-
Reaction between α-halo-nicotinic esters and a nucleophilic source such as the N-methylpyrrolidin-2-one (NMP) gave unexpected results. The presence of the halide on the pyridine gave a very interesting migration reaction. Extension to 6-methylnicotinic ester derivatives lead to an unexpected carbanion condensation.
- Kaminski, Thomas,Kirsch, Gilbert
-
p. 229 - 234
(2008/09/19)
-
- NOVEL HERBICIDES
-
Compounds of formula I: wherein R1, R2, R3, R4, m, R5, R6, n and Y are as defined in claim 1; or N-oxides, salts and optical isomers thereof. Furthermore, the present invention relates to processes for preparing compounds of formula (I), to herbicidal compositions comprising them and to methods of using them to control plants or to inhibit plant growth.
- -
-
Page/Page column 94
(2008/06/13)
-
- THERAPEUTIC PYRROLIDINES
-
The present invention provides for compounds of Formula (I), and pharmaceutically acceptable salts thereof, wherein A, J, Z, and R20 have any of the values defined therefor in the specification, and pharmaceutically acceptable salts thereof, that are useful as agents in the treatment of disorders and conditions including attention deficit hyperactivity disorder, neuropathic pain, urinary incontinence, generalized anxiety disorder, depression, schizophrenia, and fibromyalgia. Also provided are pharmaceutical compositions comprising one or more compounds of Formula (I) or pharmaceutically acceptable salts thereof.
- -
-
Page/Page column 34
(2008/06/13)
-
- Novel scaffolds for beta-helix mimicry
-
Functionalized pyridazine derivatives having a low molecular weight and pharmaceutical compositions thereof are useful as alpha-helix mimetics and for treating conditions and/or disorders mediated by alpha-helix-binding receptors and proteins.
- -
-
Page/Page column 32
(2008/06/13)
-
- Ready access to 7,8-dihydro- and 1,2,3,4-tetrahydro-1,6-naphthyridine-5(6H) -ones from simple pyridine precursors
-
Short pathways are described for the synthesis of a representative example of each of the 7,8-dihydro- and 1,2,3,4-tetrahydro-1,6-naphthyridine-5(6H)-one ring systems from simple pyridine precursors. An attempted synthesis of the related 4,6-dihydro-1,6-naphthyridin-5(1H)-one ring system from a common intermediate was unsuccessful.
- Showalter, H. D. Hollis
-
p. 1311 - 1317
(2007/10/03)
-
- NICOTINAMIDE DERIVATIVES USEFUL AS PDE4 INHIBITORS
-
This invention relates to nicotinamide derivatives of formula (I) and to pharmaceutical compositions containing, and the uses of such derivatives as PDE4 inhibitors wherein R7 is attached to the 3-or 4-position of the phenyl ring and is S(O)pR8, R8 is (C1-C4)alkyl optionally substituted by (C3-C6)cycloalkyl; m is 0 or 1; L is a (C3-C8)carbocyclic non-aromatic ring; and the remaining variables are as defined in the claims.
- -
-
Page/Page column 76
(2010/02/10)
-
- PROCESSES FOR THE PREPARATION OF N-HETEROARYL-N-ARYL-AMINES BY REACTING AN N-ARYL CARBAMIC ACID ESTER WITH A HALO-HETEROARYL AND ANALOGOUS PROCESSES
-
The present invention relates to processes for producing a diaryl amine compound of the formula (I); or a salt thereof, said process comprising the step of coupling a compound of formula (II) with an amine of formula (III) in the presence of an alkali metal salt or a transition metal catalyst, wherein: Ar1 and Ar2 are independently Q; wherein each Q is an aryl or heteroaryl ring system optionally fused to a saturated or unsaturated 5-8 membered ring having 0-4 heteroatoms; wherein Q is optionally substituted as defined in claim 1, wherein: X is a leaving group; and Y is -C(O)-O-Z; and Z is selected from C1-C6 aliphatic, benzyl, Fmoc, -SO2R’ and Q, provided that Q is not substituted with X or alkyne; wherein R’ is as defined in claim 1.
- -
-
-
- INDAZOLE DERIVATIVES THAT ARE ACTIVATORS OF SOLUBLE GUANYLATE CYCLASE
-
Compounds of formula (I) are novel indazoles useful for increasing cGMP levels in a mammal.
- -
-
Page/Page column 40-41
(2010/02/07)
-
- Antiviral agents and methods of treating viral infections
-
The present invention relates to methods of treating viral or fungal infections using 3-aminopyridine-2-carboxyaldehyde thiosemicarbazone (3-AP) and 3-amino-4-methylpyridine-2-carboxaldehyde thiosemicarbazone (3-AMP) and its prodrug forms and to pharmaceutical compositions comprising these compounds.
- -
-
-
- Modified prodrug forms of AP/AMP
-
The present invention relates to compounds according to the structure: Where R is H or CH3; R2 is phosphate which can be free acid or salt; R3 is H, F, Cl, Br, I, OCH3, OCF3, CF3 or a C1-C3 alkyl group; R4 is H, F, Cl, Br, I, OCH3, OCF3 or CF3; and R5 and R6 are each independently H, F, Cl, Br, I, OCH3, OCF3 or CF3, with the proviso that when any two of R3, R4, R5 or R6 are other than H, the other two of R3, R4, R5 or R6 are H which may be used to treat neoplasia, including cancer.
- -
-
-
- Imidazole derivatives and their use as farnesyl protein transferase inhibitors
-
The present invention relates to compounds of formula (I), wherein Ar1represents (A) and (B) or (C); R12and R13are independently hydrogen or C1-4alkyl; Ar2is phenyl or heteroaryl; p is 0 or 1; Ar3is phenyl, pyridinyl, pyridazinyl, pyrimidyl or pyrazynyl, the ring being substituted on ring carbon atoms by R2and —(CH2)nR3, and wherein Ar3is attached to Ar1C(R12)R13CH(Ar2)O— by a ring carbon atom; R2is a group of formula (2), or R2represents a lactone of formula (3), the group of formula (2) or (3) havingLorDconfiguration at the chiral alpha carbon in the corresponding free amino acid; n is 0, 1 or 2; R3is phenyl or heteroaryl; and R5-R9, m and n are as defined in the specification; or a pharmaceutically acceptable salt, prodrug or solvate thereof. Processes for their preparation, their use as therapeutic agents and pharmaceutical compositions containing them. A particular use in cancer therapy.
- -
-
Page column 52
(2010/11/29)
-
- Amino-benzocycloalkane derivatives
-
Compounds of the formula I wherein R2—C, R3—C, R4—C or R5—C may be replaced by N; and wherein n is 1, 2 or 3; R1is aryl, cycloalkyl or heterocyclyl; R2, R3, R4and R5are independently hydrogen, optionally substituted alkyl, halo, amino, substituted amino, trifluoromethyl, cyano, carboxyl, alkoxycarbonyl, aralkoxycarbonyl, (alkyl, aryl or aralkyl)-thio, (alkyl, aryl or aralkyl)-oxy, acyloxy, (alkyl, aryl or aralkyl)-aminocarbonyloxy; or any two of R2, R3, R4and R5at adjacent positions are alkylenedioxy; R6is hydrogen, optionally substituted alkyl, amino, substituted amino, acylamino, wherein Rais hydrogen or optionally substituted alkyl, Rband Rcare independently hydrogen, optionally substituted alkyl, cycloalkyl, aryl or heterocyclyl; or Rband Rctogether represent lower alkylene or lower alkylene interrupted by O, S, or N—(H, alkyl or aralkyl); Rdis optionally substituted alkyl, cycloalkyl, aryl or heterocyclyl; and Reis optionally substituted alkyl, aryl, heterocyclyl, cycloalkyl, amino or substituted amino; and pharmaceutically acceptable salts thereof; and enantiomers thereof; which are useful as inhibitors of microsomal triglyceride transfer protein (MTP) and of apolipoprotein B (ApoB) secretion.
- -
-
-
- Indium-mediated deoxygenation of amine-N-oxides in aqueous media
-
Several aromatic and aliphatic amine-N-oxides were deoxygenated to the corresponding amines in good to quantitative yield using indium metal in neutral aqueous media. Other functional groups such as alkenes, halides, esters, ethers, nitriles, amides and sulfones are unaffected under the present reaction conditions. (C) 2000 Elsevier Science Ltd.
- Yadav,Subba Reddy,Reddy, M. Muralidhar
-
p. 2663 - 2665
(2007/10/03)
-
- Isoxazole derivatives
-
An isoxazole compound having the following formula: wherein R1 represents hydrogen, halogen, alkyl, alkoxy, hydroxyl, alkylthio, amino, alkanoyl, alkanoylamino, alkanoyloxy, alkoxycarbonyl, carboxy, (alkylthio)thiocarbonyl, carbamoyl, nitro or cyano; R2 represents an amino; m is 1; n is 1 to 6; ring A represents a phenyl ring or a naphthyl ring; and X represents oxygen or sulfur. The isoxazole compound has an excellent monoamine oxidase inhibitory activity, and is useful for treating Parkinson's disease, depression and Alzheimer's disease.
- -
-
-
- Prodrug forms of ribonucleotide reductase inhibitors 3-AP and 3-AMP
-
The present invention relates to novel prodrug forms of ribonucleoside diphosphate reductase inhibitors 3-aminopyridine-2-carboxaldehyde thiosemicarbazone (3-AP) 3-amino-4-methylpyridine-2-carboxaldehyde thiosemicarbazone (3-AMP) which have increased water solubility, bioavailablity and resistance to in vivo acetylation of their amino functions. Novel compounds according to the present invention relate to those of the formula: STR1 where R4 is H or CH3 and R5 is CHR, benzyl or ortho or para substituted benzyl; R is H, CH3, CH2 CH3, CH2 CH2 CH3 or STR2 R' is a free acid phosphate, phosphate salt or an --S--S--R" group; R" is CH2 CH2 NHR6, CH2 CH2 OH, CH2 COOR7, an ortho or para substituted alkylphenyl and ortho or para substituted nitro-phenyl; R6 is H, C1 -C4 acyl group, trifluoroacetyl, benzoyl or substituted benzoyl group, and R7 is H, C1 -C4 alkyl or a benzyl or substituted benzyl.
- -
-
-
- One-pot synthesis of novel (2-Oxo-1,2-dihydropyridin-3-yl)-1,3,5- triazine derivatives from methyl 2-(N- triphenylphosphoranylidene)aminonicotinate, aryl isocyanates and primary amines: Sequential aza-wittig /cycloaddition / ring-transformation reactions
-
(2-Oxo-1,2-dihydropyridin-3-yl)-1,3,5-triazine derivatives 10 were obtained unexpectedly, in stead of pyrido[2,3-d]pyrimidine derivatives, by the intermolecular aza-Wittig reaction of methyl 2-(N- triphenylphosphoranylidene)aminonicotinate 3 with aryl isocyanates followed by attempted heterocylization by use of prim-amines. A novel sequential aza- Wittig / cycloaddition / ring-transformation mechanism for the formation of 10 has been reported based on the isolation and characterization of the key intermediates, pyrido[1,2-a][1,3,5]triazines 15 formed via [4+2] cycloaddition of the initially produced carbodiimide with aryl isocyanates.
- Okawa, Tomohiro,Osakada, Naoto,Eguchi, Shoji,Kakehi, Akikazu
-
p. 16061 - 16082
(2007/10/03)
-
- Synthesis of regioisomeric 6,9-(chlorofluoro)-substituted benzo[g]quinoline-5,10-diones, benzo[g]isoquinoline-5,10-diones and 6-chloro-9-fluorobenzo[g]quinoxaline-5,10-dione
-
Treatment of difluoro or chloro fluoro-substituted benzyl bromides 5a-c with zinc dust in tetrahydrofuran leads to the corresponding benzylic zinc bromides 6a-c. These organometallics on treatment with chlorosubstituted heterocyclic esters 4A and 4B mediated by nickel catalysis undergo couplings to yield dihalobenzyl substituted heterocyclic esters 7Aa-c and 7Ba-c. Treatment of 4c with 6c under Pd catalysis leads to 7Cc. The acids 8, prepared by hydrolysis of these esters, with treatment of fuming sulfuric acid undergo cyclizations and oxidations to yield the desired regioisomeric dihalo-substituted heterocyclic quinones 2.
- Krapcho, A. Paul,Gallagher, Cynthia E.,Hammach, Abdelhakim,Ellis, Michael,Menta, Ernesto,Oliva, Ambrogio
-
-
- Palladium(0)-catalyzed heteroarylation of 2- and 3-indolylzinc derivatives. An efficient general method for the preparation of (2-pyridyl)indoles and their application to indole alkaloid synthesis
-
Palladium(0)-catalyzed coupling of (1-(benzenesulfonyl)-2-indolyl)zinc chloride (1) and (1-(tert-butyldimethylsilyl)-3-indolyl)zinc chloride (6) with diversely substituted (alkyl, methoxy, methoxycarbonyl, nitro, hydroxy) 2-halopyridines gives the corresponding 2- and 3-(2-pyridyl)indoles [4 and 7 (or 8), respectively] in excellent yields. A series of other 3-(heteroaryl)indoles (pyrazinyl, furyl, thienyl, indolyl) have been similarly prepared from 6. The potential of some of these (2-pyridyl)indoles in alkaloid synthesis is demonstrated. Thus, from 2-(2-pyridyl)indole 4b, a new synthetic entry to the indolo[2,3-a]quinolizidine system, involving stereoselective hydrogenation of the pyridine ring with subsequent electrophilic cyclization upon the indole 3-position from an appropriately N(b)-substituted 2-(2-piperidyl)indole, is reported. For this purpose, Pummerer cyclizations have been extensively studied. Whereas the indole-unprotected sulfoxide 17 gives the corresponding indoloquinolizidine 19 in low yield and mainly undergoes an abnormal Pummerer cyclization that ultimately leads to sulfide 18, the N(a)-protected sulfoxides 24a and 24b afford the respective indoloquinolizidines 25a,b in 70% yield. On the other hand, the conversion of 3-(2-pyridyl)indole 8k into tetracyclic ketone 35 by stereoselective hydrogenation, followed by cyclization of the resulting all-cis-3-(2-piperidyl)indole 34, represents a formal synthesis of Strychnos alkaloids with the strychnan skeletal type (tubifoline, tubifolidine, 19,20-dihydroakuammicine). A similar conversion of 8j into nordasycarpidone constitutes a formal synthesis of the alkaloids of the uleine group. Reduction of nordasycarpidone leads to tetracycle 37, an advanced intermediate in a previous synthesis of tubotaiwine, a Strychnos alkaloid with the aspidospermatan skeletal type. Finally, piperidylindole 34 was transformed into tetracycle 41, an ABDE substructure of akuammiline alkaloids, by a sequence involving the skeletal rearrangement of an intermediate spiroindolenine as the crucial step.
- Amat, Mercedes,Hadida, Sabine,Pshenichnyi, Grigorii,Bosch, Joan
-
p. 3158 - 3175
(2007/10/03)
-
- Syntheses of ortho-hydroxymethylpyridinols and dioxaphosphorino[m,n-x]pyridines
-
Dioxaphosphorino[m,n-x]pyridines compounds have been prepared by condensation of methyl dichlorophosphate with new ortho-hydroxymethylpyridinols.
- Leroy,Despres,Bigan,Blondeau
-
p. 2257 - 2272
(2007/10/03)
-
- Dihydro- and tetrahydronaphthyridines
-
This invention concerns novel dihydro- and tetrahydronaphthyridines useful for enhancing the lethal effects on tumor cells to treatment causing DNA-damaging activity as with ionizing radiation or with a chemotherapeutic agent.
- -
-
-
- 2-(aza-9-fluorenonyl)carbapenem antibacterial agents
-
Carbapenems of the formula STR1 wherein a suitably substituted aza-9-fluorenone is attached at the 2-position of the carbapenem are useful antibacterial agents.
- -
-
-
- 2-(Alkylamino)nicotinic Acid and Analogs. Potent Angiotensin II Antagonists
-
A series of pyridines and other six-membered ring heterocycles connected to a biphenyltetrazole with a-CH2-NR'-link (1) were discovered to be potent angiotensin II antagonists.In the pyrimidine carboxylic acid series (W = CR, X = N, Y = CH, Z = COOH), compounds with an alkyl group (R') on the exocyclic nitrogen were much more potent than compounds with an alkyl group (R) on the heterocyclic ring.The corresponding pyridine, pyridazine, pyrazine, and 1,2,4-triazine carboxylic acids also showed potent in vitro angiotensin II antagonism.The pyridine (W, X, Y = CH, Z = COOH, R' = n-C3H7) demonstrated potent in vitro activity (pA2 = 10.10, rabbit aorta, and Ki = 0.61 nM, receptor binding in rat liver) as well as exceptional oral antihypertensive activity and bioavailability.Any nonacidic replacement for the carboxylic acid was detrimental for activity.
- Winn, Martin,De, Biswanath,Zydowsky, Thomas M.,Altenbach, Robert J.,Basha, Fatima Z.,et al.
-
p. 2676 - 2688
(2007/10/02)
-
- Processes for the preparation of morniflumate and analogous compounds
-
Novel processes for the preparation of morniflumate and analogous compounds are described, which processes allow to obtain directly the product as the free base, according to simplified synthesis schemes and in significantly higher yields than those obtained by the prior art processes. The processes of the present invention are particularly advantageous for industrial applications.
- -
-
-
- Utilizing Acetyl Hypofluorite for Chlorination, Bromination, and Etherification of the Pyridine System
-
Acetyl hypofluorite, which is easily made from F2, possesses a strong electrophilic fluorine.This electrophile is able to attach itself to the nitrogen atom of pyridine and activate the ring toward nucleophilic attacks.The ultimate elimination of HF results in an overall easy nucleophilic displacement of the hydrogen of the important 2-position .The nucleophiles used: Clδ-, Brδ-, ROδ-, originate from solvents such as CH2Cl2, CH2Br2, and various primary alcohols.Thus, 2-halo- or 2-alkoxypyridines were formed.The reaction conditions (room temperature, very short reaction times, and good yields) transform the task of direct substitution of the pyridine ring from an extremely difficult to a very easy procedure.
- Hebel, David,Rozen, Shlomo
-
p. 6298 - 6301
(2007/10/02)
-
- Atypical Antipsychotic Agents: Patterns of Activity in a Series of 3-Substituted 2-Pyridinyl-1-piperazine Derivatives
-
A series of 3-substituted 2-pyridinyl-1-piperazine derivaties have been appended to cyclic imide groups and evaluated for their potential antipsochotic activity.The dopamine receptor affinities of these target molecules, as well as their ability to block apomorphine-induced stereotypy or reverse neuroleptic-induced catalepsy, was dependent on the lipophilic and electronic characteristics of the substituent situated on the pyridine ring.Groups with +? and -? values were most consistent with the desired biological profile of the target molecules, the cyano moiety being the optimum choice.Evaluation of compound 12 in a monkey model of amphetamine psychosis, and the regional selectivity it expresses for the A10 dopaminergic cell bodies in electrophysiological experiments, suggest this compound would be an atypical antipsychotic agent with few side effects.
- New, James S.,Yevich, Joseph P.,Temple, Davis L.,New, Kimberly B.,Gross, Sharon M.,et al.
-
p. 618 - 624
(2007/10/02)
-
- Antisecretory 4-oxy-3-carboxy or cyano-1,2-dihydro-2-oxo-1,8-naphthyridine derivatives
-
Substituted 4-oxy-3-carboxy or cyano-1,2-dihydro-2-oxo-1,8-naphthyridine derivatives as gastric antisecretory agents for use in the treatment of peptic ulcer disease.
- -
-
-