- Studying Histone Deacetylase Inhibition and Apoptosis Induction of Psammaplin A Monomers with Modified Thiol Group
-
Psammaplin A (PsA) is a bromotyrosine disulfide dimer with histone deacetylase (HDAC) inhibition and acts through reduced monomer PsA-SH. We studied the connection of HDAC inhibition, cell growth inhibition, and apoptosis induction of PsA-SH by modifying the -SH group with deletion (6a) or replacement with hydroxamic acid (10b) or benzamide (12g). PsA-SH inhibits HDAC1/2/3 and 6a loses the HDAC inhibition ability. 10b inhibits HDAC1/2/3/6 while 12g shows selective inhibition of HDAC3. PsA-SH and 10b, but neither 6a nor 12g, induce apoptosis in human leukemia HL-60 cells associated with increased acetylation of Histone H3. PsA-SH and 10b inhibit growth of several solid tumor cell lines in vitro and Lewis lung cancer cell growth in vivo. PsA-SH is a simple scaffold for developing selective HDAC inhibitors and induces apoptosis through inhibiting HDAC1/2.
- Bao, Yu,Xu, Qihao,Wang, Lin,Wei, Yunfei,Hu, Baichun,Wang, Jian,Liu, Dan,Zhao, Linxiang,Jing, Yongkui
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- MACROCYCLIC COMPOUND AS CDK INHIBITOR, PREPARATION METHOD THEREFOR, AND USE THEREOF IN MEDICINE
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The present invention relates to a macrocyclic compound as a CDK inhibitor, a preparation method therefor and the use thereof in medicine. Specifically, the present invention relates to a novel macrocyclic compound represented by a general formula (I), a preparation method therefor, a pharmaceutical composition containing the compound, the use thereof as a therapeutic agent, particularly as a CDK inhibitor, and the use thereof in treating cancers, inflammation, viral infections, cardiac hypertrophy or HIV, wherein each substituent of the general formula (I) is the same as that defined in the description.
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Paragraph 0083; 0138; 0139
(2021/08/19)
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- Stereoselective Syntheses of trans-Anhydromevalonic Acid and trans-Anhydromevalonyl Group-Containing Natural Products
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Collective total syntheses of trans-anhydromevalonic acid (tAHMA) and trans-anhydromevalonyl (tAHM) group-containing natural products (pestalotiopin A, pestalotiopamide C, pestalotiopamide D, farinomalein E, eleutherazine B, and trichocyclodipeptide A) were achieved using tAHMA esters as key intermediates. To this end, tAHMA tert-butyl ester was newly prepared by Z-vinyltosylation of tert-butyl 3-oxo-5-((triisopropylsilyl)oxy)pentanoate followed by the Negishi cross-coupling reaction with Me2Zn. tAHMA esters were converted to the target natural products via esterification or amidation. Comparison of the spectroscopic data of synthetic and natural products confirmed the E-configuration of the tAHM moieties in the natural products.
- Kitsuwa, Kohei,Nakayama, Atsushi,Okamura, Hironori,Saito, Kai,Shinada, Tetsuro,Yamamoto, Yuki,Yasuno, Yoko
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- Manufacturing method for 3-(2-chloropropionylamino)propionic acid alkyl ester
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A process for the preparation 3 - (2- chloropropionylamino) propionic acid alkyl esters. The process of the present invention uses alkylacrylates differently than those using β - alanine as a starting material. 3 - (2-chloropropionylamino) propionic acid alkyl ester, which is an intermediate of a uracil compound useful as a herbicide, can be obtained in high yield and high purity without the need for a step of producing a β-alanine methyl ester hydrochloride.
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Paragraph 0024-0028
(2021/01/01)
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- Resveratrol amino acid ester derivative and preparation method thereof
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The invention discloses a resveratrol amino acid ester derivative and a preparation method thereof, and belongs to the technical field of fine chemical substance synthesis. The structure of the resveratrol amino acid ester derivative is represented by a formula shown in the description. The resveratrol amino acid ester derivative is synthesized from resveratrol, R amino acid, R' alcohol, dichlorosulfoxide and di(p-nitrobenzene) carbonate with 4-dimethylaminopyridine (DMAP) as a catalyst and acetonitrile as a solvent, wherein the R amino acid is one of alpha-alanine, beta-alanine and gamma-aminobutyric acid, and the R' alcohol is one of methanol, ethanol and n-propanol. The technical problem that resveratrol is difficult to preserve is solved, the pharmacological toxicity introduced by a resveratrol substituent group is lowered, and the resveratrol amino acid ester derivative has the pharmaceutical effects of resveratrol and amino acid. It is expected that the above novel compound playsa great role in beauty treatment and production of fatigue-relieving and blood pressure-lowering medicines.
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Paragraph 0059; 0070-0075
(2019/07/04)
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- Amido Complexes of Iridium with a PNP Pincer Ligand: Reactivity toward Alkynes and Hydroamination Catalysis
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The pincer ligand HN(CH2CH2PPh2)2 (1; PNHP) reacted with [{Ir(μ-X)(cod)}2] (X = Cl, OMe), affording complexes [fac-(PNHP)Ir(cod)]Cl (2) and [fac-(PNP)Ir(cod)] (3), respectively. The X-ray molecular structure of 2 showed that the PNP ligand coordinates in a facial fashion, with the N atom in an axial site and both P atoms coordinated in the equatorial plane. Compound 1 is able to protonate the hydroxo bridges in the complex [{Ir(μ-OH)(coe)2}2] forming the new amido complex [mer-(PNP)Ir(coe)] (4). Complex 4 is an extremely air sensitive compound, as confirmed by the isolation of the oxo complex [mer-(PNP)Ir(σ2-O2)] (8) from its interaction with air. Protonation of 4 with HBF4 afforded the corresponding amino complex [mer-(PNHP)Ir(coe)]BF4 (5), whose molecular structure enlightened by X-ray crystallography confirmed the PNP ligand to be coordinated in a meridional fashion. The coe ligand in 4 is tightly bonded to iridium; however, under an atmosphere of ethylene at 60 °C or with acrylonitrile at 70 °C complex 4 exchanges the olefin, affording compounds [mer-(PNP)Ir(σ2-C2H4)] (6) and [mer-(PNP)Ir(σ2-C2H3CN)] (7), respectively. Interaction of 4 with alkynes depends on the nature of the substrate; therefore, methyl phenylpropiolate reacted with 4, affording the adduct [mer-(PNP)Ir(σ2-PhCCC(O)OMe)] (9), while the parent acetylene undergoes a double C-H activation, affording the Ir(III) complex [fac-(PNHP)IrH(Ca‰?CH)2] (10). A DFT theoretical analysis of this transformation supports a metal-ligand cooperation mechanism. The reaction starts by deprotonation of an alkyne moiety by the PNP ligand followed by oxidative addition of the C-H bond to the metal of a second alkyne molecule. Additionally, we have tested complex 4 as a catalyst for the addition of gaseous ammonia to activated unsaturated substrates. A DFT theoretical analysis disclosed the operative mechanism on these organic transformations, which starts with a nucleophilic attack of ammonia to the bound alkyne, hydrogen migration to the metal, and reductive elimination steps.
- Hermosilla, Pablo,López, Pablo,García-Ordunìa, Pilar,Lahoz, Fernando J.,Polo, Víctor,Casado, Miguel A.
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p. 2618 - 2629
(2018/08/21)
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- 4-Connected azabicyclo[5.3.0]decane Smac mimetics-Zn2+ chelators as dual action antitumoral agents
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Putative dual action compounds (DACs 3a–d) based on azabicyclo[5.3.0]decane (ABD) Smac mimetic scaffolds linked to Zn2+-chelating 2,2′-dipicolylamine (DPA) through their 4 position are reported and characterized. Their synthesis, their target a
- Manzoni, Leonardo,Samela, Alessandro,Barbini, Stefano,Cairati, Silvia,Penconi, Marta,Arosio, Daniela,Lecis, Daniele,Seneci, Pierfausto
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supporting information
p. 2336 - 2344
(2017/05/10)
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- Synthesis and biological evaluation of analogues of the marine cyclic depsipeptide obyanamide
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On the basis of the total synthesis of obyanamide, 20 analogues of this marine cyclic depsipeptide have been synthesized by (i) preparation of the tripeptide fragments in the western hemisphere using Z/OtBu protocol; (ii) preparation of the dipeptide fragments in the eastern hemisphere using Boc/OMe protocol; and (iii) fragments coupling, removal of protecting groups (Boc and OtBu, in one pot), and macrocyclizaion in the last step. The cytotoxic test showed that three synthetic compounds exhibited moderate activities against HL-60, KB, LOVO, and A549 cell lines. According to the results, the β-amino acid residue was found to play a critical role in the biological activities. Additionally, the ester bond along with the Ala(Thz) moiety was also essential for biological activities. However, it seems too early to draw a conclusion that the N-methylation of Val/Phe can lead to higher or lower cytotoxic activities.
- Zhang, Wei,Ding, Ning,Li, Yingxia
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experimental part
p. 533 - 539
(2012/05/04)
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- 2-Oxo-2H-benzo[h]benzopyran as a new light sensitive protecting group for neurotransmitter amino acids
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Aiming at the development of new benzopyran-based photocleavable protecting groups, novel chloromethylated and hydroxymethylated 2-oxo-2H-benzo[h] benzopyran derivatives bearing a methoxy substituent were designed and used in the synthesis of a series of fluorescent bioconjugates, by linking through an ester or urethane bond to several model neurotransmitter amino acids (glycine, alanine, β-alanine and γ-aminobutyric acid, GABA). The resulting fluorescent bioconjugates with emission in the visible range and high fluorescent quantum yields, were subjected to photocleavage reaction in methanol/HEPES buffer (80:20) solution at different wavelengths of irradiation (250, 300, 350 and 419 nm) and photocleavage kinetic data were obtained.
- Soares, Ana M. S.,Costa, Susana P. G.,Goncalves, M. Sameiro T.
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experimental part
p. 121 - 133
(2010/09/07)
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- Supramolecular gelation of alcohol and water by synthetic amphiphilic gallic acid derivatives
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The supramolecular organogelation of alcohols was observed in relatively hydrophobic amphiphiles with a short oligo(ethylene glycol) unit and three long alkyl chains at room temperature, while the hydrogelation occurred in more hydrophilic gelators with a longer poly(ethylene glycol) unit and two long alkyl chains at various temperatures. When a hot aqueous solution of some of the synthetic hydrogelators was cooled down, the supramolecular hydrogel was formed at room temperature. In some other amphiphiles with less intermolecular interactivity in water at room temperature, a reverse phase transition of sol to gel was observed by elevating the temperature of their aqueous systems, especially below a physiological temperature, 37 °C. The supramolecular hydrogelation at a low or high temperature was dependent on a slight molecular modification of the synthetic amphiphiles.
- Tamiaki, Hitoshi,Ogawa, Keishiro,Enomoto, Keisuke,Taki, Kazutaka,Hotta, Atsushi,Toma, Kazunori
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supporting information; experimental part
p. 1661 - 1666
(2010/04/24)
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- PYRROLINE DERIVATIVES AGAINST CELL RELEASING TUMOR NECROSIS FACTOR, PREPARATION METHODS AND USES THEREOF
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Compounds represented by Formula (I) or Formula (II) against cell releasing TNFα, their pharmaceutically acceptable salts or hydrates and preparation methods and uses thereof, in which A and B represent CH2, CO, SO, or SO2; D represents S, NH, or NC1-6 alkyl; R1 represents H, or one or two same or different radical(s) selected from the group consisting of F, Cl, Br, C1-4 alkyl,OH,OC1-4 alkyl,NO2,NHC(O)C1-4 alkyl,NH2,NH(C1-4 alkyl), or N(C1-4 alkyl)2.
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Page/Page column 13
(2009/08/14)
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- Phosphorylthioureas and phosphorylureas containing amino acid fragments
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A series of (dialkoxyphosphoryl)thioureas and their 1,3,2-oxazaphosphinane analogs containing fragments of glycine, alanine, ss-alanine, L-aspartic and L-glutamic acids, as well as phosphorylureas derived from glycine and ss-alanine were synthesized in the search for potential biologically active compounds (including possible inhibitors of aspartate trans-carbamoylase).
- Shipov,Genkina,Petrovskii
-
p. 2512 - 2516
(2014/05/06)
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- PYRIMIDINE DERIVATIVES AS PROTEIN KINASE INHIBITORS
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The present invention relates to a compound of formula (VII)I, or a pharmaceutically acceptable salt or ester thereof, wherein: X is NR7; Y is O or N-(CH2)nR19; n is 1, 2 or 3; m is 1 or 2; R1 and Rs
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Page/Page column 44; 75
(2009/05/29)
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- THIAZOLYL-DIHYDRO-CHINAZOLINE
-
Disclosed are compounds of general formula (I), wherein the groups A, R1, R2, Ra and Rb have the meanings given in the claims and specification, the tautomers, racemates, enantiomers, diastereomers and the mixtures thereof, and optionally the pharmacologically acceptable acid addition salts, solvates and hydrates thereof, and processes for preparing these thiazolyl-dihydro-quinazolines and the use thereof as pharmaceutical compositions.
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Page/Page column 25
(2008/06/13)
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- New approaches for the synthesis of isotopically labelled guanidine-derived amino acids and noradrenaline reuptake inhibitors
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A new approach for the stereoselective synthesis of guanidine-derived amino acids, L-arginine and (+)-blastidic acid, has been devised which allows the selective incorporation of isotopic labels in both the side chain of the amino acid as well as the guanidine unit. A new asymmetric synthesis of the (S,R)-diastereomer of reboxetine, an antidepressant, has also been completed which allows the specific incorporation of radiolabelled iodine for SPECT imaging. Copyright
- Bischoff, Roland,Hamilton, Deborah J.,Jobson, Nicola K.,Sutherland, Andrew
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p. 323 - 326
(2008/02/05)
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- COMPOUNDS AS COR5 ANTAGONISTS
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The present invention discloses the compounds of formula I or their pharmaceutically acceptable salts, which are useful as CCR5 antagonists. The preparation and use of the compounds of formula I, pharmaceutical composition containing the same are also dis
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-
Page/Page column 10
(2010/11/26)
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- Lipases in β-dipeptide synthesis in organic solvents
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A number of β-dipeptides were prepared by two-step lipase-catalyzed reactions where N-acetylated β-amino esters were first activated as 2,2,2-trifluoroethyl esters with Candida antarctica lipase B (CAL-B). The activated esters were then used to acylate a
- Li, Xiang-Guo,Kanerva, Liisa T.
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p. 5593 - 5596
(2007/10/03)
-
- THIAZOLE DERIVATIVES AND USE THEREOF
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The present invention is related to thiazole derivatives of Formula (I) in particular for the treatment and/or prophylaxis of autoimmune disorders and/or inflammatory diseases, cardiovascular diseases, neurodegenerative diseases, bacterial or viral infections, kidney diseases, platelet aggregation, cancer, transplantation, graft rejection or lung injuries.
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Page/Page column 87
(2008/06/13)
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- A highly efficient, asymmetric synthesis of blastidic acid: The β-amino acid component of the antibiotic, (+)-blasticidin S
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A new approach for the asymmetric synthesis of blastidic acid, the β-amino acid component of the antibiotic, (+)-blasticidin S has been achieved in 11 steps and 30% overall yield. The key transformations involve a one-pot Swern/Wittig reaction sequence to
- Bischoff, Roland,McDonald, Niall,Sutherland, Andrew
-
p. 7147 - 7149
(2007/10/03)
-
- Glutaryl Acylases: One-Reaction Enzymes or Versatile Enantioselective Biocatalysts?
-
A significant broad substrate specificity, that crosses over the usual β-lactam derivatives, has been observed with an industrial glutaryl-7-aminocephalosporanic acid acylase (GA). This enzyme possesses significant enantioselective amidase and even esterase activity, with a stereopreference for the S-enantiomer. The easy separation of products from unreacted reagents, possessing different physical-chemical properties, is achieved by solvent extraction, avoiding chromatography or distillation during reaction work-up.
- Raimondi, Stefano,Monti, Daniela,Pagnoni, Ugo Maria,Riva, Sergio
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p. 783 - 789
(2007/10/03)
-
- Synthesis of β-amino arylketones through the addition of ArLi derivatives to β-aminoesters
-
2-Lithiumthiophene and 2-lithiumpyridine were allowed to react with N-substituted β-aminoesters. Only β-amino arylketones were obtained from N-BOC, N-H derivatives, while arylenoates were formed (retro-conjugate addition) from those substrates bearing N-Bn, N-H substituents, despite the aryllithium used. When the nitrogen is disubstituted (BOC and Bn), the product distribution depended on the nucleophile, leading to tertiary alcohols for 2-lithiumthiophene or ketones for 2-lithiumpyridine. Tertiary alcohols were also formed when PhLi was used as a nucleophile.
- Lima, Paulo G.,Sequeira, Lucia C.,Costa, Paulo R.R.
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p. 3525 - 3527
(2007/10/03)
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- Artificial trinuclear metallopeptidase synthesized by cross-linkage of a molecular bowl with a polystyrene derivative
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A novel methodology is reported for construction of active sites of artificial multinuclear metalloenzymes: Transfer of metal-chelating sites confined in a prebuilt cage to a polymeric backbone. Artificial active sites comprising two or three moieties of Cu(II) complex of tris(2-aminoethyl)amine (tren) were prepared by transfer of Cu(II)tren units confined in a molecular bowl (MB) to poly(chloromethylstyrene-co-divinylbenzene) (PCD). By treatment of unreacted chloro groups of the resulting PCD with methoxide and destruction of the MB moieties attached to PCD with acid followed by addition of Cu(II) ion to the exposed tren moieties, catalytic polymers with peptidase activity were obtained. The average number (β) of proximal Cu(II)tren moieties in the active site of the artificial multinuclear metallopeptidase was determined by quantifying the Cu(II) content. Several species of the artificial metallopeptidases with different β contents were prepared and examined for catalytic activity in hydrolysis of various cinnamoyl amide derivatives. The PCD-based catalytic polymers did not hydrolyze a neutral amide but effectively hydrolyzed carboxyl-containing amides (N-cinnamoyl glycine, N-cinnamoyl β-alanine, and N-cinnamoyl γ-amino butyrate). Analysis of the kinetic data revealed that the active sites comprising three Cu(II)tren units were mainly responsible for the catalytic activity. When analyzed in terms of k(cat), the catalytic activity of the PCD-based artificial peptidase was comparable to or better than the catalytic antibody with the highest peptidase activity reported to date. A mechanism is suggested for the effective cooperation among the three metal centers of the active site in hydrolysis of the carboxyl-containing amides.
- Moon, Sung-Ju,Jeon, Joong Won,Kim, Heesuk,Suh, Myunghyun Paik,Sun, Junghun
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p. 7742 - 7749
(2007/10/03)
-
- Bleomycin model complex bearing a carbamoyl derived substituent capable of coordination to the chelated metal ion as a sixth ligand
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A new, simple bleomycin (BLM) model compound bearing a carbamoyl group mimicking BLM's sugar-tagged carbamoyl moiety was synthesized and the physicochemical properties of its divalent metal complexes were studied. The Fe complex of the model compound exhi
- Arai, Takayuki,Shinozuka, Kazuo,Sawai, Hiroaki
-
-
- Efficient lanthanide catalysis in aminoacyl-transfer from the bipyridine-functionalized amide-substrate to alcohols at ambient temperature
-
Lanthanide cations showed high catalytic activities in aminoacylation of alcohols by the amide-substrates having bipyridine as a metal chelation site at 30°C (first-order rate constants were 10-4 s-1 range at Ce3+/substrate = 0.2), yielding corresponding amino acid esters almost quantitatively.
- Araki, Koji,Kajikawa, Takeshi,Kawaguchi, Satoshi
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p. 295 - 296
(2007/10/03)
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- MICHAEL-TYPE ADDITION OF DIETHYL PHOSPHORAMIDATE TO α,β-UNSATURATED ESTERS
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Michael-type addition of diethyl phosphoramidate to α,β-unsaturated esters occurs when the reactants are refluxed in toluene or xylene with an excess of potassium carbonate in the presence of tetrabutylammonium bromide (TBABr).Dephosphorylation of methyl and ethyl acrylate adducts leads to the respective β-alanine esters. Key words: Diethyl phosphoramidate; α,β-unsaturated esters; Michael-type addition; β-alanine esters; phase-transfer catalysis.
- Osowska-Pacewicka, K.,Zawadzki, S.,Zwierzak, A.
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-
- Preferential Formation of Amino Acid Esters in Aqueous Alcohol Solutions: Solvolysis of 6,6'-Bis(aminoacylamino)-2,2'-bipyridine by Metal Coordination
-
Exclusive formation of amino acid esters took place at an appreciable rate in the CuII-catalysed solvolysis of 6,6'-(α-alanylamino or α-phenylalanylamino)-2,2'-bipyridine in alcohol-borate buffer (pH 7.2) solutions at 20 deg C via formation of an amide-O-coordinated complex, even though appreciable amounts of water (0-40percent v/v) were present in the solution.
- Araki, Koji,Kuboki, Takashi,Yamada, Masaki,Shiraishi, Shinsaku
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p. 1060 - 1062
(2007/10/02)
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- Design of Potent Protein Kinase Inhibitors Using the Bisubstrate Approach
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A new class of serine/threonine protein kinase inhibitors was designed by associating, in the same structure, mimics of both the ATP binding site and a protein substrate.Among the several potent antagonists which were obtained, the most active consists of isoquinoline-5-sulfonamide, as ATP mimic, and Ser-Arg6, as peptidic moiety, bound by a -NH(CH2)2NH(CH2)2CO- linker.This compound, with a Ki of 0.1 μM toward protein kinase C (PKC) and 0.004 μM toward cyclic AMP dependent protein kinase (PKA), is respectively 60- and 750-fold more active than the commercial inhibitor H-7.
- Ricouart, A.,Gesquiere, J. C.,Tartar, A.,Sergheraet, C.
-
-
- One-Carbon Compounds as Synthetic Intermediates. The Synthesis of Hydropyrimidines and Hydroquinazolines by Sequential Nucleophilic Addition to Diphenyl Cyanocarbonimidate with Concomitant Cyclization
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Diphenyl cyanocarbonimidate (1) undergoes nucleophilic addition with ω-amino esters and amines in a sequential manner to give guanidine derivatives that, for the most part, spontaneously cyclize to give hydropyrimidines or hydroquinazolines.The hydropyrimidines could be dehydrogenated to dihydropyrimidines, and the NCN group could be hydrolyzed to a carbonyl or amine group in the pyrimidine and to an amine group in the quinazoline series.The regiospecificity of the cyclization was determined by a combination of spectroscopic methods and comparison of compounds synthesized by standard routes.The scope of the synthetic route is indicated.Some of the acyclic N-cyano-O-phenylisoureas formed by the first nucleophilic addition exist as mixtures of isomers, and the barriers to interconversion have been determined by NMR spectroscopy.
- Garratt, Peter J.,Hobbs, Christopher J.,Wrigglesworth, Roger
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p. 1062 - 1069
(2007/10/02)
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- A Facile Synthesis of α-Amino Esters via Reduction of α-Nitro Esters Using Ammonium Formate as a Catalytic Hydrogen Transfer Agent
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Various nitroesters 3 were selectively and rapidly reduced to their corresponding amino esters 4 in very good yield using anhydrous ammonium formate as a catalytic hydrogen transfer agent.
- Ram, Siya,Ehrenkaufer, Richard E.
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p. 133 - 135
(2007/10/02)
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- HYDROLYSIS OF ESTERS OF N-RETINYLIDENEAMINO ACIDS
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The hydrolysis rate of the ester bond in the molecules of methyl esters of the N-retinylidene derivatives of aliphatic amino acids depends on their chain lengths.The higher reaction rates for the derivatives of γ-aminobutyric and δ-aminovaleric acids are explained by intramolecular catalysis.
- Karpenko, E. P.,Mitsner, B. I.,Zvonkova, E. N.,Evstigneeva, R. P.
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p. 1669 - 1673
(2007/10/02)
-
- Antibacterial 3-(5-tetrazolyl)penam compounds
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Certain novel 6-acylamino-2,2-dimethyl-3-(5-tetrazolyl)penam derivatives, and salts thereof; their use as broad-spectrum antibacterial agents; and methods for their preparation. Their preparation comprises acylation of the novel intermediate, 6-amino-2,2-dimethyl-3-(5-tetrazolyl)penam or simple derivatives thereof, followed, in some cases, by further transformations of the 6-acylamino group or by removal of a protecting group from the 5-tetrazolyl moiety. Process for the preparation of 6-amino-2,2-dimethyl-3-(5-tetrazolyl)penam, simple derivatives thereof and intermediates therefor.
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- Antibacterial 3-(5-tetrazolyl) penam compounds
-
Certain novel 6-acylamino-2,2-dimethyl-3-(5-tetrazolyl)penam derivatives, and salts thereof; their use as broad-spectrum antibacterial agents; and methods for their preparation. Their preparation comprises acylation of the novel intermediate, 6-amino-2,2-dimethyl-3-(5-tetrazolyl)penam or simple derivatives thereof, followed, in some cases, by further transformations of the 6-acylamino group or by removal of a protecting group from the 5-tetrazolyl moiety. Process for the preparation of 6-amino-2,2-dimethyl-3-(5-tetrazolyl)penam, simple derivatives thereof and intermediates therefor.
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-
- L-Pyroglutamyl-L-histidyl-L-prolyl-beta-alaninamide and salts
-
This disclosure relates to L-pyroglutamyl-L-histidyl-L-prolyl-beta-alaninamide and acid addition salts thereof as anti-depressant agents.
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-
- Process for production of 6-amino-2,2-dimethyl-3-(5-tetrazolyl)penam and certain derivatives thereof
-
A chemical process which comprises reacting 6-(2-phenylacetamido)- or 6-(2-phenoxyacetamido)-2,2-dimethyl-3-(5-tetrazolyl)penams and certain derivatives thereof which carry a blocking or pseudo blocking group on the tetrazolyl moiety with a halogenating agent at or below 0° C. to form the corresponding imino halide, followed by reaction of the imino halide with an alcohol below about -20° C. to form the corresponding imino ether, and hydrolyzing the imino ether under acid conditions. The preparation of the starting 6-acyl-2,2-dimethyl-3-(5-tetrazolyl)penams is described.
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