240401-28-9

Basic information

• Product Name: 7-Boc-2-hydroxy-7-azaspir...
• Synonyms: 7-Boc-2-hydroxy-7-azaspir...;7-Boc-2-hydroxy-7-azaspiro[3.5]nonane;7-Tert-butoxycarbonyl-7-azaspiro[3.5]nonan-2-ol;2-Hydroxy-7-aza-spiro[3.5]nonane-7-carboxylic acid tert-butyl ester;tert-Butyl 2-hydroxy-7-azaspiro[3.5]nonane-7-carboxylate - B7194
• CAS NO: 240401-28-9
• Molecular Formula: C₁₃H₂₃NO₃
• Molecular Weight: 241.32662
• Mol File: 240401-28-9.mol

Chemical Properties

• Boiling Point: 350.7±42.0 °C(Predicted)
• Appearance: /
• Density: 1.12±0.1 g/cm3(Predicted)
• Storage Temp.: Sealed in dry,Room Temperature
• PKA: 14.99±0.20(Predicted)
• CAS DataBase Reference: 7-Boc-2-hydroxy-7-azaspir...(CAS DataBase Reference)
• NIST Chemistry Reference: 7-Boc-2-hydroxy-7-azaspir...(240401-28-9)
• EPA Substance Registry System: 7-Boc-2-hydroxy-7-azaspir...(240401-28-9)

Safety Data

• Hazardous Substances Data: 240401-28-9(Hazardous Substances Data)

Usage

Uses

Used in Medicinal Chemistry:
7-Boc-2-hydroxy-7-azaspiro[2.4]heptane-2-carboxylic acid is used as a building block for the development of pharmaceuticals and biologically active molecules. Its Boc protecting group allows for mild deprotection to reveal the free amine, facilitating the synthesis of various compounds with potential therapeutic applications.
Used in Organic Synthesis:
In the field of organic synthesis, 7-Boc-2-hydroxy-7-azaspiro[2.4]heptane-2-carboxylic acid serves as a valuable intermediate due to its unique structure and functional groups. The presence of the Boc protecting group and the hydroxy group at the 2-position enables the synthesis of diverse compounds for a wide range of applications.
Used in Drug Development:
7-Boc-2-hydroxy-7-azaspiro[2.4]heptane-2-carboxylic acid is utilized in drug development as a key intermediate in the synthesis of pharmaceuticals. Its ability to be deprotected and further modified makes it a versatile component in the creation of new drug candidates with potential therapeutic benefits.
Used in Chemical Research:
In the realm of chemical research, 7-Boc-2-hydroxy-7-azaspiro[2.4]heptane-2-carboxylic acid is employed as a subject of study to explore its properties, reactivity, and potential applications in various chemical processes. Understanding its behavior can lead to the discovery of new synthetic routes and applications in different industries.

Upstream product

• 203661-69-2 tert-butyl 2-oxo-7-azaspiro[3.5]nonane-7-carboxylate 
• 159635-49-1 tert-butyl 4-methylidenepiperidine-1-carboxylate 
• 396653-31-9 tert-butyl 1,1-dichloro-2-oxo-7-azaspiro[3.5]nonane-7-carboxylate 

Downstream Products

• 1256240-59-1 3-methylcarbamoyl-isoxazol-5-ylmethyl 2-(4-chlorophenoxy)-7-aza-spiro[3.5]nonane-7-carboxylate 
• 1256240-60-4 3-carbamoyl-isoxazol-5-ylmethyl 2-(4-chlorophenoxy)-7-aza-spiro[3.5]nonane-7-carboxylate 
• 1256241-03-8 2-(4-chlorophenoxy)-7-aza-spiro[3.5]-nonane 
• 1256241-04-9 3-ethoxycarbonyl-isoxazol-5-ylmethyl 2-(4-chlorophenoxy)-7-aza-spiro[3.5]nonane-7-carboxylate 
• 1421270-68-9 C₂₄H₂₆Cl₂FN₅O 
• 1421270-73-6 (R)-tert-butyl 2-(4-(6-amino-5-((R)-1-(2,6-dichloro-3-fluorophenyl)ethoxy)pyridin-3-yl)-1H-pyrazol-1-yl)-7-azaspiro[3.5]nonane-7-carboxylate 
• 1448850-36-9 tert-butyl 2-(4-amino-3-(4-phenoxyphenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)-7-azaspiro[3.5]nonane-7-carboxylate 
• 203662-66-2 2-cyano-7-azaspiro[3.5]nonane-7-carboxylic acid tert-butyl ester 
• 587869-08-7 7-aza-spiro[3.5]nonane-2-ol hydrochloride 
• 1239319-82-4 2-amino-7-aza-spiro[3.5]nonane-7-carboxylic acid tert-butyl ester 
• 1558037-98-1 tert-butyl 2-(tosyloxy)-7-azaspiro[3.5]nonane-7-carboxylate 

Relevant articles and documents

Stereoselective Diboration of Spirocyclobutenes: A Platform for the Synthesis of Spirocycles with Orthogonal Exit Vectors

The diastereo- and enantioselective diboration of spirocyclobutenes provides a platform for the rapid preparation of a wide variety of chiral spirocyclic building blocks. The chemoselective functionalization of the carbon-boron bond in the products, including a stereospecific sp3-sp2 Suzuki–Miyaura cross-coupling reaction, provides a powerful tool to control the directionality and the nature of the exit vectors in the spirocyclic framework.

Regioselective Monoborylation of Spirocyclobutenes

We present a strategy for the synthesis of spirocyclic cyclobutanes with modulable exit vectors based on the regioselective monoborylation of spirocyclobutenes. Using an inexpensive copper salt and a commercially available bidentate phosphine, a broad variety of borylated spirocycles have been prepared with complete regiocontrol. The boryl moiety provides a synthetic handled for further functionalization, allowing access to a wide array of spirocyclic building blocks from a common intermediate.

ANTAGONISTS OF THE MUSCARINIC ACETYLCHOLINE RECEPTOR M4

Disclosed herein are substituted 7-azaspiro[3.5]nonane compounds, which may be useful as antagonists of the muscarinic acetylcholine receptor M4 (mAChR M4). Also disclosed herein are methods of making the compounds, pharmaceutical co

BENZO RING DERIVATIVE WITH B2 RECEPTOR AGONIST AND M3 RECEPTOR ANTAGONIST ACTIVITIES AND USE THEREOF IN MEDICINE

A compound represented by general formula (I), or a stereoisomer, a hydrate, a metabolite, a solvate, a pharmaceutically acceptable salt, a cocrystal, or a prodrug thereof, the preparation method thereof, and use thereof in the manufacture of a medicament for treatment of an airway obstructive disease, wherein the substituents are defined as in the specification.

FXR receptor modulator, and preparation method and application thereof

The invention discloses a FXR receptor modulator, and a preparation method and application thereof, belonging to the field of pharmaceutical chemistry. The FXR receptor modulator with structural characteristics as shown in a formula I which is described i

1-azaspirocycle compound, and preparation method and applications thereof

The invention discloses a 1-azaspirocycle compound, and preparation method and applications thereof, and belongs to the field of pharmaceutical chemistry. The 1-azaspirocycle compound with a structurerepresented by formula I, or a pharmaceutically acceptable salt or a stereisomer or a solvate or a prodrug thereof is capable of realzing combination with Autotaxin, can be taken as an Autotaxin inhibitor, and can be used for prevention and treatment of diseases with Autotaxin expression increasing pathological characteristics such as cancer and fibrosis diseases especially pulmonary fibrosis andhepatic fibrosis, metabolic diseases, myelodysplastic syndrome, cardiovascular diseases, autoimmune diseases, inflammation, neurological diseasses, or pain. Compared with single component inhibitors,the 1-azaspirocycle compound and the derivatives possesses following advantages: blocking and interfacing at the upsteam of a plurality of key signal channels are realized, tumor cell growth and transfer are relieved or dalyed, early caused drug resistance is avoided, and novel means are provided for treatment of tumor cells.

FXR RECEPTOR MODULATOR, PREPARATION METHOD THEREFOR, AND USES THEREOF

The present disclosure disclosed a modulator of FXR receptor and preparation and use thereof, which relates to the technical filed of medicinal chemistry. The present disclosure provides a modulator of FXR receptor having a structural formula I or a pharmaceutically acceptable salt, stereoisomer, solvate or prodrug thereof, which can combine with FXR receptor (that is NR1H4) and be acted as a FXR agonist or a partial agonist for preventing and treating the disease mediated by FXR, such as chronic intrahepatic or extrahepatic cholestasis, hepatic fibrosis caused by chronic cholestasis or acute intrahepatic cholestasis, chronic hepatitis B, gallstone, hepatic carcinoma, colon cancer or intestinal inflammatory disease, etc. Specifically, for some chemical compounds, their EC50 for FXR agonist activity reach below 100nM, which show an excellent FXR agonist activity and an excellent prospect to provide a new pharmaceutical selection in clinical treatment for the disease mediated by FXR.

Synthesis of Electron-Deficient Heteroaromatic 1,3-Substituted Cyclobutyls via Zinc Insertion/Negishi Coupling Sequence under Batch and Automated Flow Conditions

Synthesis of 1,3-substituted cyclobutyls enabled by zinc insertion into functionalized iodocyclobutyl derivatives followed by Negishi coupling with halo-heteroaromatics is reported. Two distinct sets of conditions were developed; the first involved a two-step batch protocol using activated Rieke zinc, and the second involved a multistep continuous flow process. Both methods showed complementarity and allowed for rapid access to these medicinally relevant motifs, the possibility of scaling up, and automation for library synthesis.

ANTIBACTERIAL COMPOUNDS

The present invention relates to the following compounds, wherein the integers are as defined in the description, and where the compounds may be useful as medicaments, for instance for use in the treatment of tuberculosis.

Synthetic methods of 7-azaspiro[3,5]-nonane-2-ol and hydrochloride compound thereof

The invention discloses 7-azaspiro-[3,5]-nonane-2-ol and a hydrochloride compound thereof. Concretely, N-Boc-4-piperidone is used as a raw material, a wittig reaction is carried out in order to prepare N-Boc-4-methylenepiperidine, zinc/copper is used for catalysis of trichloroacetyl chloride in order to carry out [2+2] cyclisation for preparing N-Boc-7-azaspiro ketone; the azaspiro ketone intermediate is reduced into N-Boc-7-azaspiro-ol by sodium borohydride at a room temperature, and finally 2mol/L hydrochloric acid-ethyl acetate is used for removing Boc in order to prepare a target product hydrochloride whose purity reaches 98%. The product has the advantages of economical and easily available reagents and raw materials which are needed, simple operation, and high product purity; and the product is suitable for batch production.