Search results for "domino"

ChemInform Abstract: Asymmetric Tandem Reactions: New Synthetic Strategies

2010

The use of domino and multicomponent reactions in asymmetric synthesis is con- stantly increasing nowadays. This allows for the synthesis of complex molecules in a single synthetic sequence, usually with high atom economy. Herein, we report three examples of new asymmetric tandem reactions recently developed in our laboratories, giving rise to new families of enantiomerically enriched fluorinated and nonfluorinated heterocycles. Thus, 1,4-dihydropyridines (1,4-DHPs) bearing fluorinated substituents at C6 were assembled by means of a Hantzsch-type reaction; cyclic β-amino carbonyl derivatives were prepared using a cross-metathesis (CM)-intramolecular aza-Michael sequence; while fluorinated i…

An unexpected Dimroth rearrangement leading to annelated thieno[3,2-d][1,2,3]triazolo[1,5-a]pyrimidines with potent antitumor activity.

2013

An unusual Dimroth rearrangement occurring in the reaction leading to annelated thieno[2,3-e][1,2,3]triazolo[1,5-a]pyrimidine core allowed the isolation of the linear isomer thieno[3,2-d][1,2,3]triazolo[1,5-a]pyrimidine. By decorating the linear isomer with the same chains that improved the biological activity of the angular isomers, new annelated thieno[3,2-d][1,2,3]triazolo[1,5-a]pyrimidines were designed and synthesized. They were selected by the Developmental Therapeutics Program (DTP) of the National Cancer Institute (NCI) for the anticancer screening against a panel of 60 human tumor cell lines. The biological results showed that the new derivatives exhibited strong antiproliferative …

New annelated thieno[2,3-e][1,2,3]triazolo[1,5-a]pyrimidines, with potent anticancer activity, designed through VLAK protocol

2012

Drug design was performed through the Virtual Lock-and-Key (VLAK) protocol. This in silico approach allowed to select new annelated thienotriazolopyrimidine derivatives, potentially antitumor drugs. Starting from benzothieno[2,3-e][1,2,3]triazolo[1,5-a]pyrimidine and Pyrido[3',2':4,5]thieno[2,3-e][1,2,3]triazolo[1,5-a]pyrimidine core structures, new derivatives of these nuclei were designed and synthesized. Three of them were selected by the Development Therapeutical Program (DTP) of the National Cancer Institute (NCI) for the anticancer screening against a panel of 60 human tumor cell lines. The biological results showed that the new derivatives exhibited an excellent antiproliferative act…

Diastereoselective Synthesis of Spiro[pyrazolone-4,3′-tetrahydrothiophenes] via a Sulfa-Michael/Aldol Domino Reaction

2016

Synthesis : journal of synthetic organic chemistry 48(23), 4091-4098(2016). doi:10.1055/s-0035-1562473

N‐Heterocyclic Carbene Catalyzed Quadruple Domino Reactions: Asymmetric Synthesis of Cyclopenta[ c ]chromenones

2018

An N-heterocyclic carbene catalyzed domino sequence via α,β-unsaturated acyl azolium intermediates has been developed. This strategy provides a convenient enantioselective route to functionalized tricyclic coumarin derivatives and cyclopentanes. DFT studies and control experiments were performed to gain better insight into the reaction mechanism.

Rektummelanome – Stellenwert der modernen Therapie

2008

Rectal melanoma is a rare disease. There is much controversy concerning cause, incidence and treatment of the disease and the spreading of recurrence. In this article, we discuss actual aspects of diagnostic, therapy and prognosis on the basis of our series of seven patients as well as a literature review. The surgical therapy in the form of local tumour excision with a disease-free margin of up to 1-2 cm is the initial therapeutic modality of choice. Large tumours that obviously could not be removed in sano should be treated with a multimodal concept. Such tumours should be treated by a combination of neoadjuvant radiation and chemotherapy for down-staging with subsequent local excision (L…

The Ruthenium‐Catalyzed Domino Cross Enyne Metathesis/Ring‐Closing Metathesis in the Synthesis of Enantioenriched Nitrogen‐Containing Heterocycles

2020

Transsacral rectocele following combined neurinoma resection: A case report

2015

Highlights • Case of a combined (transsacral and laparoscopic) resection of a presacral tumour. • First described case of a transsacral rectocele two years after this procedure. • Possibility of laparoscopic defect repair of transsacral defects.

La rappresentanza apparente: verso un nuovo modello di rappresentanza

2022

ABSTRACT RAPPRESENTATNZA APPARENTE L’autore propone una ricostruzione della rappresentanza apparente, in grado di avallare il consolidamento di un modello uniforme di rappresentanza e di imputazione dei rapporti giuridici, fondato sull’agire per conto altrui e sul principio di affidamento. Seguendo autorevoli insegnamenti, che attribuivano all’agire nell’interesse altrui la base sostanziale dell’istituto rappresentativo, l’autore individua diverse forme di agire rappresentativo, il cui dato comune sarebbe dato dall’agire per conto altrui e dal principio di affidamento. Nonostante lo schema disegnato dall’art. 1388 c.c. descriva una fattispecie caratterizzata dalla presenza dei requisiti del…

Asymmetric tandem reactions: New synthetic strategies

2010

The use of domino and multicomponent reactions in asymmetric synthesis is constantly increasing nowadays. This allows for the synthesis of complex molecules in a single synthetic sequence, usually with high atom economy. Herein, we report three examples of new asymmetric tandem reactions recently developed in our laboratories, giving rise to new families of enantiomerically enriched fluorinated and nonfluorinated heterocycles. Thus, 1,4-dihydropyridines (1,4-DHPs) bearing fluorinated substituents at C6 were assembled by means of a Hantzsch-type reaction; cyclic β-amino carbonyl derivatives were prepared using a cross-metathesis (CM)–intramolecular aza-Michael sequence; while fluorinated ind…