20655-61-2

Upstream product

• 100-88-9 cyclohexylsulfamic acid 
• 78441-82-4 3-{2-[(5-dimethylaminomethyl-furan-2-yl)methylthio]ethylamino}-4-amino-1,2,5-thiadiazole 1-oxide 
• 7778-42-9 sulphamoyl chloride 
• 90-05-1 2-methoxy-phenol 
• 136167-44-7 3-(2-methoxyphenoxy)propan-1-ol 
• 627-18-9 1-bromo-3-propanol 
• 108-93-0 cyclohexanol 

Downstream Products

• 1306748-15-1 cyclohexyl N-(cyclohex-2-en-1-yl)sulfamate 

Relevant academic research and scientific papers

Intermolecular amination of allyl alcohols with sulfamates: Effective utilization of mercuric catalyst

Herein, we describe the intermolecular amination of allyl alcohols with sulfamates, which have been underutilized as nitrogen nucleophiles for allylic amination. Methyl sulfamate is a good nucleophile in the presence of mercuric triflate and efficiently generates monoallylation products in excellent yield at room temperature. Furthermore, the solid-supported mercuric catalyst silaphenyl mercuric triflate also showed remarkable catalytic activity for the allylic amination. Intermolecular amination of allyl alcohol with sulfamate as a modifiable nitrogen nucleophile is presented. Mercuric reagents act as highly efficient catalyst for the allylic amination, and the procedure was applied to the preparation of various amine derivatives. In many cases, the reaction can be carried out at room temperature and is applicable to a large range of allylic alcohols to give the monoallylated products in excellent yield. Copyright

Carbonic Anhydrase Inhibitors: Inhibition of Transmembrane, Tumor-Associated Isozyme IX, and Cytosolic Isozymes I and II with Aliphatic Sulfamates

A series of aliphatic sulfamates and related derivatives incorporating cyclic/polycyclic (steroidal) moieties in their molecules has been synthesized and assayed as inhibitors of the zinc enzyme carbonic anhydrase (CA) and, more precisely, of the cytosolic isozymes CA I and II and the transmembrane, tumor-associated isozyme CA IX. The most potent CA I inhibitor was n-tetradecyl sulfamate and some (substituted)benzyl/phenethyl sulfamates (inhibition constants in the low micromolar range). Against CA II, low nanomolar inhibitors (0.7-3.4 nM) were n-decyl sulfamate and the (substituted)benzyl/phenethyl derivatives mentioned above. Effective CA II inhibition was also observed for the hydroxy/keto derivatives of dehydroepiandrosterone sulfamate. Efficient CA IX inhibitory properties, with inhibition constants in the range of 9-23 nM, were observed for the aliphatic sulfamates C10-C16 (with the most potent inhibitor being the n-dodecyl derivative) and the (substituted)benzyl/phenethyl sulfamates. The inhibition profile of the three investigated isozymes with this type of compound was rather different, allowing us to hope that the preparation of CA IX-selective inhibitors is possible (selectivity ratios toward hCA IX versus hCA II in the range of 5-63 has been observed for some of these compounds, whereas for the clinically used sulfonamides this parameter is in the range of 0.23-0.51). These data are critical for the design of novel antitumor therapies, mainly for hypoxic tumors that overexpress CA IX, which are nonresponsive to radiation or chemotherapy.

Compounds having one or more aminosulfaonyloxy radicals useful as pharmaceuticals

Methods of treating chronic arthritis and osteoporosis which utilize both known and novel compounds which would fall under the general formula:(HO)p--A--[--OS(O) 2 NR 1 R 2 ] zwherein A encompasses a wide range of values including but not limited to aryl, loweralkyl, cycloalkyl, and carbohydrates including sucrose and fructose; p is equal to the number of unreacted hydroxy groups contained on the molecule and may be zero; z is the number of --OS(O) 2 NR 1 R 2 groups and is always at least one; R 1 and R 2 are selected from hydrogen, loweralkyl, carboxy and the like; a novel process for preparing the compounds is provided wherein an appropriate sulfamic acid aryl ester is reacted with a hydroxy substituted A radical which may or may not contain thereon protected carboxyl, amino or hydroxy substituents, in an aprotic solvent containing a tertiary amine base. Pharmaceutical compositions for the treatment of chronic arthritis and osteoporosis are also provided.

SUBSTITUTED 3,4-DIAMINO-1,2,5-THIADIAZOLES HAVING HISTAMINE H2-RECEPTOR ANTAGONIST ACTIVITY

Histamine H 2-receptor antagonists of the formula STR1 wherein A, m, Z, n and R 1 are as defined herein, and their nontoxic pharmaceutically acceptable salts are novel anti-ulcer agents which are prepared by ring closure of a substituted ethanediimidamide of the formula STR2

INTERMEDIATES FOR PREPARING 3,4-DIAMINO-1,2,5-THIADIAZOLES

Histamine H 2-receptor antagonists of the formula STR1 wherein A, m, Z, n and R 1 are as defined herein, and their nontoxic pharmaceutically acceptable salts, hydrates and solvates are novel anti-ulcer agents which are prepared by ring closure of a substi

Substituted 3,4-diamino-1,2,5-thiadiazoles having histamine H2 -receptor antagonist activity

Histamine H2 -receptor antagonists of the formula STR1 wherein A, m, Z, n and R1 are as defined herein, and their nontoxic pharmaceutically acceptable salts, hydrates and solvates are novel anti-ulcer agents which are prepared by rin

PROCESS FOR PREPARING 1,2,5-THIADIAZOLES

Histamine H 2-receptor antagonists of the formula STR1 wherein A, m, Z, n and R 1 are as defined herein, and their nontoxic pharmaceutically acceptable salts, hydrates and solvates are novel anti-ulcer agents which are prepared by ring closure of a substi

α-{[(Arylalkyl)amino]alkyl}-4-hydroxy-3-(lower-alkylsulfinyl)benzenemethanols

The instant invention is directed to α-(aminoalkyl)-4-hydroxy-3-(alkylsulfinylbenzenemethanols and to a method of utilizing the compounds for reducing blood pressure in mammals.