Solid-Phase Synthesis of 2,4-Diaminoquinazoline Libraries

Dener, Jeffrey M.; Lease, Timothy G.; Novack, Aaron R.; Plunkett, Matthew J.; Hocker, and Michael D.; Fantauzzi, Pascal P.

doi:10.1021/cc010027u

Cited by 17 publications

(7 citation statements)

References 16 publications

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“…Dener et al developed the synthesis of 2,4-diaminoquinazoline on modified Merrifield resin. 126 ■ SOLID-PHASE SYNTHESIS OF THIAZOLOPYRIMIDINES Thiazolopyrimidine derivatives are mainly used in biomedical industries. Thiazolopyrimidines are a major component of various biologically active molecules and are used in the treatment of arthritis, multiple sclerosis, asthma, etc.…”

Section: Acs Combinatorial Sciencementioning

confidence: 99%

Advances in the Solid-Phase Synthesis of Pyrimidine Derivatives

Aparna

Devaky

2019

ACS Comb. Sci.

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This Review describes the existing synthetic approaches for the solid-phase synthesis (SPS) of differently substituted and fused pyrimidine derivatives. These synthetic strategies are classified on the basis of the different synthetic routes leading to the particular type of pyrimidine heterocycle formed. The Review discusses the application of a variety of polystyrene derived supports for the construction of pyrimidine rings. The effect of microwave heating on the solid-phase synthesis is also addressed in the review.

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Section: Acs Combinatorial Sciencementioning

confidence: 99%

Advances in the Solid-Phase Synthesis of Pyrimidine Derivatives

Aparna

Devaky

2019

ACS Comb. Sci.

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“…Dener and co-workers [44] have also been reported a solid-phase synthesis of 2,4-diaminoquinazoline (43) starting from polymer bound amines (40). The key steps included, reaction of the polymer-bound amine (40) with 6,7-dimethoxy-2,4-dichloroquinazoline followed by the displacement of the second chlorine with an amine and subsequent cleavage to afford the product (43) as shown in Scheme 6.…”

Section: Quinazolinementioning

confidence: 99%

Recent Advances in the Solid-Phase Combinatorial Synthetic Strategies for the Quinoxaline, Quinazoline and Benzimidazole Based Privileged Structures

Kamal¹,

Reddy²,

Devaiah

et al. 2006

MRMC

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Quinoxaline, quinazoline and benzimidazole based templates have been synthesized on solid-support employing different methodologies. This review enlightens academic and industrial examples of combinatorial synthesis for this type of heterocycles that appeared in the literature in the last decade. Hence, some of the important synthetic strategies for the generation of quinoxaline, quinazoline and benzimidazole based privileged structures, and the important biological activities for these heterocycles have been highlighted. Further, benzothiadiazinone, thioxoquinazolinone, cinnoline and indazole are also examined in this review.

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“…A more general and versatile method was described by Dhanoa et al [42] and later slightly modified by Dener et al [43]. The starting material was represented by polymer bound amines (48) which reacted with 6,7-dimethoxy-2,4-dichloroquinazoline followed by an aromatic nucleophilic substitution with the appropriate amine and subsequent cleavage to give the desired quinazoline (51) (Figure 8) A modified synthesis of the antihypertensive agent iodoazidoarylprazosin (52) [44] (Figure 1) has been published recently.…”

Section: Synthesis Of Prazosin Derivativesmentioning

confidence: 99%

Recent advances in the design and synthesis of prazosin derivatives

Minarini¹,

Bolognesi²,

Tumiatti³

et al. 2006

Expert Opinion on Drug Discovery

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Due to the large number of therapeutic indications, particularly for antagonists, a field of constant interest in medicinal chemistry is the design, synthesis and pharmacological evaluation of ligands that bind at α1-adrenoreceptors, which include α1a, α1b and α1d subtypes. This review, which is mainly based on literature over the past 10 years, focuses on the developments of some of the most potent, selective and widely used α1-adrenoreceptor antagonists that are structurally related to prazosin (which is characterised by a quinazoline moiety). Initially introduced in therapy for the management of hypertension, prazosin derivatives have become increasingly common in the treatment of benign prostatic hyperplasia. During the past few years, new perspectives have emerged for the use of these derivatives as a novel class of apoptosis-inducing agents in prostate cancer.

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Solid-Phase Synthesis of 2,4-Diaminoquinazoline Libraries

Cited by 17 publications

References 16 publications

Advances in the Solid-Phase Synthesis of Pyrimidine Derivatives

Advances in the Solid-Phase Synthesis of Pyrimidine Derivatives

Recent Advances in the Solid-Phase Combinatorial Synthetic Strategies for the Quinoxaline, Quinazoline and Benzimidazole Based Privileged Structures

Recent advances in the design and synthesis of prazosin derivatives

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